Therapeutic: Urinary Tract Stimulants Pharmacologic: Cholinergic

CHOLINERGIC DRUGS AFFECTING AUTONOMIC NERVOUS SYSTEM
A. Cholinergic Drugs
Cholinergic drugs are a wide variety of drugs used to work on the parasympathetic nervous system. These drugs work by enhancing the
actions of acetylcholine, a neurotransmitter or chemical messenger in the brain. Effects of increased acetylcholine are considered the
everyday work of the body, such as salivation, digestion, and skeletal muscle relaxation.
1. Bethanicol (be-than-e-kole)
Duvoid, Urabeth, Urecholine
Classification
Therapeutic: Urinary tract stimulants
Pharmacologic: Cholinergic
Pregnancy Category C
Indications
Postpartum and postoperative non obstructive urinary retention or urinary retention caused by neurogenic
bladder.
Action
Stimulates cholinergic receptors. Effects include: Contraction of the urinary bladder, decreased bladder capacity, increased frequency of
ureteral peristaltic waves, increased tone and peristalsis in the GI tract, increased pressure in the lower esophageal sphincter, increased gastric
secretions. Therapeutic Effects: Bladder emptying.
Pharmacokinetics
Absorption: Poorly absorbed after oral administration, requiring larger doses by mouth than subcutaneously.
Distribution: Does not cross the blood-brain barrier.
Metabolism and Excretion: Unknown.
Half-life: Unknown.
TIME/ACTION PROFILE (response on bladder muscle)
ROUTE ONSET PEAK DURATI
ON
PO 30–90min 1hr 6hr
Subcut 5–15min 15–30min 2hr
Contraindications/Precautions
Contraindicated in: Hypersensitivity; Mechanical obstruction of the GI or GU tract.
Use Cautiously in: History of asthma; Ulcer disease; Cardiovascular disease; Epilepsy; Hyperthyroidism; Sensitivity to cholinergic agents or
effects; OB, Lactation, Pedi: Safety not established.
Adverse Reactions/Side Effects
CNS: headache, malaise. EENT: lacrimation, miosis. Resp: bronchospasm. CV: HEART BLOCK, SYNCOPE/CARDIAC ARREST,
bradycardia, hypotension. GI: abdominal discomfort, diarrhea, nausea, salivation, vomiting. GU: urgency. Misc: flushing, sweating,
hypothermia.
Interactions
Drug-Drug: Quinidine and procainamide may antagonize cholinergic effects. Additive cholinergic effects with cholinesterase inhibitors. Use
with ganglionic blocking agents may result in severe hypotension. Do not use with depolarizing neuromuscular blocking agents. Effectiveness
will be decreased by anticholinergics.
Drug-Natural Products: Cholinergic effects may be antagonized by angel’s trumpet, jimsonweed, or scopolia.
Route/Dosage
PO (Adults): 25–50mg 3 times daily. Dose may be determined by administering 5– 10mg q 1–2hr until response is obtained or total of 50 mg
administered or by starting with 10mg, giving 25mg 6hr later, then, if needed, 50mg 6hr later. PO(Children): 0.2mg/kg 3 times daily or
0.15mg/kg 4 times daily.
Subcut (Adults): 5mg 3–4 times daily. Dose may be determined by administering 2.5mg q 15–30 min until response is obtained or total of 4
doses administered.
Subcut (Children): 0.06mg/kg 3 times daily or 0.05mg/kg 4 times daily.
NURSING IMPLICATIONS
Assessment
● Monitor BP, pulse, and respirations before administering and for at least 1hr after subcut administration.
● Monitor intake and output ratios. Palpate abdomen for bladder distention. Notify physician or other health care professional if drug fails to
relieve condition for which it was prescribed. Catheterization may be ordered to assess post void residual.
● Lab Test Considerations: May cause an increase in serum AST, amylase, and lipase concentrations.
● Toxicity and Overdose: Observe patient for drug toxicity (sweating, flushing, abdominal cramps, nausea, salivation). If over dosage occurs,
treatment includes atropine sulfate (specific antidote).
Potential Nursing Diagnoses
Impaired urinary elimination (Indications)
Implementation
● A test dose is usually employed before maintenance to determine minimum effective dose.
● Oral and subcut doses are not interchangeable.
● PO: Administer medication on an empty stomach, 1hr before or 2 hr after meals, to prevent nausea and vomiting.
● Subcut: Parenteral solution is intended only for subcut administration. Do not give IM or IV. In advertent IM or Iv administration may cause
cholinergic overstimulation (circulatory collapse, drop in BP, abdominal cramps, bloody diarrhea, shock, and cardiac arrest).
● Do not use if solution is discolored or contains a precipitate.
Patient/Family Teaching
● Instruct patient to take medication exactly as directed. Missed doses should be taken as soon as possible within 2hr; otherwise, return to
regular dosing schedule. Do not double doses.
● Caution patient to change positions slowly to minimize orthostatic hypotension.
● Advise patient to report abdominal discomfort, salivation, sweating, or flushing to health care professional.
Evaluation/Desired Outcomes
● Increase in bladder function and tone.
2. Physostigmine (fi-zoe-stig-meen)
Antilirium
Classification
Therapeutic: antidotes
Pharmacologic:cholinergics, anticholinesterases
Indications
Reversal of CNS effects due to over dose of drugs capable of causing the anticholinergic syndrome, including: belladonna or other plant
alkaloids, phenothiazines, tricyclic antidepressants, antihistamines (reverses delirium, hallucinations, coma, and some arrhythmias, but not
completely effective in reversing cardiac conduction defects or tachycardia). Action Inhibits the breakdown of acetylcholine so that it
accumulates and has a prolonged effect. Result is generalized cholinergic response, including: Miosis, Increased tone of intestinal and skeletal
musculature, Bronchial and ureteral constriction, Bradycardia, Increased salivation, Lacrimation, Sweating, CNS stimulation.
Therapeutic Effects: Reversal of anticholinergic excess.
Pharmacokinetics
Absorption: Readily absorbed from subcut and IM sites.
Distribution: Widely distributed; crosses the blood-brain barrier.
Metabolism and Excretion: Metabolized by cholinesterases present in many tissues. Small amounts excreted unchanged in the urine.
Half-life: 1–2hours.
TIME/ACTION PROFILE (systemic cholinergic effects=miosis)
ON
IM, IV 3–8min unknown 45–60min
Contraindicated in: Hypersensitivity; Hypersensitivity to bisulfites; Gangrene; Asthma; Diabetes; Cardiovascular disease; Mechanical
obstruction of the GI or GU tract; Any vagotonic state; Concurrent use of choline esters or depolarizing neuromuscular blocking agents
(decamethonium, succinylcholine); Lactation: Discontinue medication or bottle feed; Pedi: Preparations containing benzyl alcohol should be
avoided in newborns to prevent potentially fatal gasping syndrome.
Use Cautiously in: Ulcer disease; Epilepsy; Hyperthyroidism. Exercise Extreme Caution in: Pregnancy or lactation (10–20%ofnewborns will
suffer from muscle weakness; use only if clearly indicated); Children (reserve for life-threatening situations).
CNS: seizures, restlessness, dizziness, hallucinations, weakness. EENT: lacrimation, miosis. Resp: bronchospasm, excess respiratory
secretions. CV: bradycardia, hypotension. GI: abdominal cramps, diarrhea, nausea, vomiting, excess salivation. Derm: rash.
Interactions
Drug-Drug: Prolongs action of depolarizing muscle-relaxing agents (succinylcholine, decamethonium); avoid concurrent use. Cholinergic
effects may be antagonized by other drugs possessing anticholinergic properties, including antihistamines, antidepressants, atropine,
haloperidol, phenothiazines, quinidine, and disopyramide.
Drug-Natural Products: Angel’s trumpet, jimson weed, and scopolia may antagonize cholinergic effects. Route/Dosage
IM, IV (Adults): Anticholinergic toxicity—2 mg initially; may be repeated as symptoms recur. Postanesthesia—0.5–1mg; may be repeated q
10–30 min.
IM, IV (Children):20mcg/kg; may repeat every 5–10 min as needed (up to 2mg total dose).
Assessment
● Monitor pulse, respiratory rate, and BP frequently throughout parenteral administration. Monitor ECG during IV administration.
● Anticholinergic Excess: Monitor neurologic status frequently. Institute seizure precautions Protect patient from self-injury that may be
caused by CNS effects of overdose.
Toxicity and Overdose: Overdose is manifested by bradycardia, respiratory distress, seizures, weakness, nausea, vomiting, stomach cramps,
diarrhea, diaphoresis, and increased salivation and tearing.
● Atropine is the antidote.
● Treatment of over dose includes establishing an airway and supporting ventilation, atropine sulfate 2–4 mg (may be repeated every 3–10 min
to control muscarinic effects),pralidoxime chloride 50–100 mg/min (to control neurologic and skeletal muscle effects), and supportive therapy.
Risk for injury (Indications)
Implementation
IV Administration
● Direct IV: Repeated doses may be needed because of short duration of action. Rate: May be given through Y-site at a rate of no more than 1
mg over 1 min (0.5 mg over 1 min for children). Rapid administration may cause bradycardia; increased salivation, which can lead to
respiratory distress; or seizures.
● Anticholinergic Excess: Explain purpose of medication and need for close monitoring. Evaluation/Desired Outcomes
● Reversal of CNS symptoms secondary to anticholinergic excess resulting from drug over dose or ingestion of poisonous plants.
B. Anticholinergic
If cholinergic drugs work to enhance the parasympathetic nervous system, then anticholinergic drugs work to enhance the sympathetic
nervous system. By blocking acetylcholine from sending chemical messages, anticholinergic drugs cause a decrease in parasympathetic
effects. The results of blocking parasympathetic effects are referred to as anticholinergic effects, and they include: reduced smooth muscle
spasm, reduced digestive tract movement, pupil dilation, and decreased production of secretions, increased heart rate, airway relaxation, and
reduced urine output.
1)Atropine (at-ro-peen)
Atro-Pen
Classification Therapeutic: antiarrhythmics
Pharmacologic: anticholinergics, antimuscarinics
Indications
IM: Given preoperatively to decrease oral and respiratory secretions. IV: Treatment of sinus bradycardia and
heart block. IV: Reversal of adverse muscarinic effects of anticholinesterase agents (neostigmine,
physostigmine, orpyridostigmine). IM, IV: Treatment of anticholinesterase (organophosphate pesticide)
poisoning. Inhaln: Treatment of exercise-induced bronchospasm.
Action
Inhibits the action of acetylcholine at postganglionic sites located in: Smooth muscle, Secretory glands, CNS (antimuscarinic activity). Low
doses decrease: Sweating, Salivation, Respiratory secretions. Intermediate doses result in: Mydriasis (pupillary dilation), Cycloplegia (loss of
visual accommodation), Increased heart rate. GI and GU tract motility are decreased at larger doses.
Therapeutic Effects: Increased heart rate. Decreased GI and respiratory secretions. Reversal of muscarinic effects. May have a spasmolytic
action on the biliary and genitourinary tracts.
Pharmacokinetics
Absorption: Well absorbed following subcut or IM administration.
Distribution: Readily crosses the blood-brain barrier. Crosses the placenta and enters breastmilk. Metabolism and Excretion: Mostly
metabolized by the liver; 30–50% excreted unchanged by the kidneys.
Half-life: Children 2yr: 4–10hr; Children 2yr:1.5–3.5hr; Adults:4–5hr.
TIME/ACTION PROFILE (inhibition of salivation)
ON
IM, subcut rapid 15–50min 4–6hr
IV immediate 2–4min 4–6hr
Contraindicated in: Hypersensitivity; Angle-closure glaucoma; Acute hemorrhage; Tachycardia secondary to cardiac insufficiency or
thyrotoxicosis; Obstructive disease of the GI tract.
Use Cautiously in: Intra-abdominal infections; Prostatic hyperplasia; Chronic renal, hepatic, pulmonary, or cardiac disease; OB, Lactation:
Safety note stablished; IV administration may produce fetal tachycardia; Pedi: Infants with Down syndrome have increased sensitivity to
cardiac effects and mydriasis. Children may have increased susceptibility to adverse reactions. Exercise care when prescribing to children with
spastic paralysis or brain damage; Geri: Increased susceptibility to adverse reactions.
Adverse Reactions/Side EffectsCNS: drowsiness, confusion, hyperpyrexia. EENT: blurred vision, cycloplegia, photophobia, dry eyes,
mydriasis. CV: tachycardia, palpitations, arrhythmias. GI: dry mouth, constipation, impaired GI motility. GU: urinary hesitancy, retention,
impotency. Resp: tachypnea, pulmonary edema. Misc: flushing, decreased sweating.
Interactions
Drug-Drug: increase anticholinergic effects with other anticholinergics, including antihistamines, tricyclic antidepressants, quinidine, and
disopyramide. Anticholinergics may alter the absorption of other orally administered drugs by slowing motility of the GI tract. Antacids
decrease absorption of anticholinergics. May increase GI mucosal lesions in patients taking oral potassium chloride tablets. May alter response
to beta-blockers.
Route/Dosage Pre anesthesia (To Decrease Salivation/Secretions)
IM, IV, Subcut (Adults): 0.4–0.6mg 30–60 min pre-op.
IM, IV, Subcut (Children >5kg): 0.01–0.02mg/kg/dose 30–60 min pre-op to a maximum of 0.4mg/dose; minimum:0.1mg/dose.
IM, IV, Subcut (Children <5kg): 0.02mg/kg/dose 30–60 min pre-op then q 4–6 hr as needed.
Bradycardia
IV (Adults):0.5–1mg; may repeat as needed q 5 min, not to exceed a total of 2mg (q3–5 min in Advanced Cardiac Life Support guidelines) or
0.04mg/kg (total vagolytic dose).
IV (Children): 0.02mg/kg (maximum single dose is 0.5mg in children and 1mg in adolescents); may repeat q 5min up to a total dose of 1mg
in children (2mg in adolescents).
Endo tracheal (Children): use the IV dose and dilute before administration.
Reversal of Adverse Muscarinic Effects of Anticholinesterases
IV (Adults): 0.6–12mg for each 0.5–2.5mg of neostigmine methylsulfate or 10– 20mg of pyridostigmine bromide concurrently with
anticholinesterase.
Organophosphate Poisoning
IM(Adults): 2mg initially, then 2mg q 10 min as needed up to 3 times total.
IV(Adults): 1–2mg/dose q 10–20 min until atropinic effects observed then q 1–4 hr for 24 hr; up to 50mg in first 24 hr and 2g over several
days may be given in severe intoxication.
IM (Children>10yr >90lbs): 2mg.
IM (Children 4–10yr 40–90lbs): 1mg.
IM (Children 6mo–4yr 15–40lbs): 0.5mg.
IV(Children): 0.02–0.05mg/kg q 10–20min until atropinic effects observed then q1–4hr for 24hr.
Bronchospasm
Inhaln (Adults): 0.025–0.05mg/kg/dose q 4–6hr as needed; maximum 2.5mg/ dose.
Inhaln (Children): 0.03–0.05 mg/kg/dose 3–4 times/day; maximum 2.5 mg/ dose.
Assessment
● Assess vital signs and ECG tracings frequently during IV drug therapy. Report any significant changes in heart rate or BP, or increased
ventricular ectopy or angina to health care professional promptly.
● Monitor intake and output ratios in elderly or surgical patients because atropine may cause urinary retention.
● Assess patients routinely for abdominal distention and auscultate for bowel sounds. If constipation becomes a problem, increasing fluids and
adding bulk to the diet may help alleviate constipation.
● Toxicity and Overdose: If over dose occurs, physostigmine is the antidote.
Decreased cardiac output (Indications)
Impaired oral mucous membrane (Side Effects)
Constipation (Side Effects)
Implementation
● IM: Intense flushing of the face and trunk may occur 15–20min following IM administration. In children, this response is called “atropine
flush” and is not harmful.
IV Administration
● Direct IV: Diluent: Administer undiluted. Rate: Administer over1 min; more rapid administration may be used during cardiac resuscitation
(follow with 20mL saline flush). Slow administration (over >1min) may cause a paradoxical bradycardia (usually resolved in approximately
2min).
● Y-Site Compatibility:abciximab, alfentanyl, amikacin, aminophylline, amiodarone, argatroban, ascorbic acid, azathioprine, aztreonem,
benztropine, bivalirudin, bumetanide, buprenorphine, butorphanol, calcium chloride, calcium gluconate, cefazolin, cefoperazone, cefotaxime,
cefotetan, cefoxitin, ceftazidime, ceftriaxone, cefuroxime, chloramphenicol, chlorpromazine, clindamycin, cyanocobalamin, cyclosporine,
dexamethasone, dexmedetomidine, digoxin, diphenhydramine, dobutamine, dopamine, doripenem, doxycycline, enalaprilat, ephedrine,
epinephrine, epoetin alfa, eptifibatide, erythromycin, esmolol, etomidate, famotidine, fenoldopam, fentanyl, fluconazole, folic acid,
furosemide, ganciclovir, gentamicin, glycopyrrolate, heparin, hydrocortisone sodium succinate, hydromorphone, imipenem/cilastatin,
indomethacin, insulin, isoproterenol, ketamine, ketorolac, labetalol, lidocaine, magnesium sulfate, mannitol, meperidine, meropenem,
methadone, methyldopate, methylprednisolone, metoclopramide, metoprolol, midazolam, morphine, multivitamins, nafcillin, nalbuphine,
naloxone, nitroglycerin, nitroprusside, norepinephrine, ondansetron, oxacillin, oxytocin, palonosetron, papaverine, penicillin G, pentamidine,
pentazocine, pentobarbital, phenobarbital, phentolamine, phenylephrine, phytonadione, potassium chloride, procainamide, prochlorperazine,
promethazine, propranolol, protamine, pyridoxime, ranitidine, sodium bicarbonate, streoptkinase, succinylcholine, sufentanil, theophylline,
thiamine, ticarcillin/clavulanate, tirofiban, tobramycin, tolazoline, vancomycin, vasopressin, verapamil, vitamin B complex with C.
● Y-Site Incompatibility: amphotericin B colloidal, dantrolene, diazepam, diazoxide, pantoprazole, phenytoin, trimethoprim/sulfamethoxazole,
thiopental.
● Endotracheal: Dilute with 5–10mL of 0.9% NaCl.
● Rate: Inject directly in to the endotracheal tube followed by several positive pressure ventilations. Patient/Family Teaching
● May cause drowsiness. Caution patients to avoid driving or other activities requiring alertness until response to medication is known.
● Instruct patient that oral rinses, sugarless gum or candy, and frequent oral hygiene may help relieve dry mouth.
● Caution patients that atropine impairs heat regulation. Strenuous activity in a hot environment may cause heat stroke. Advise patient to
notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult with health care
professional before taking other medications.
● Pedi: Instruct parents or caregivers that medication may cause fever and to notify health care professional before administering to a febrile
child.
● Geri: Inform male patients with benign prostatic hyperplasia that atropine may cause urinary hesitancy and retention. Changes in urinary
stream should be reported to health care professional. Evaluation/Desired Outcomes
● Increase in heartrate.
● Dryness of mouth.
● Reversal of muscarinic effects.
2. Aricept
donepezil (doe-nep-i-zill)
Classification
Therapeutic: anti-Alzheimer’s agents
Pharmacologic:cholinergics (cholinesterase inhibitors)
Indications
Mild, moderate, or severe dementia/neuro cognitive disorder associated with Alzheimer’s disease.
Action
Inhibits acetylcholinesterase thus improving cholinergic function by making more acetylcholine
available.
Therapeutic Effects: May temporarily lessen some of the dementia associated with Alzheimer’s disease. Enhances cognition. Does not cure
the disease.
Pharmacokinetics
Absorption: Well absorbed after oral administration.
Distribution: Unknown. Protein Binding: 96%.
Metabolism and Excretion: Partially metabolized by the liver (CYP2D6 and CYP3A4 enzymes) and partially excreted by kidneys (17%
unchanged). Two metabolites are pharmacologically active.
Half-life:70hr.
TIME/ACTION PROFILE (improvement in symptoms)
ROUT ONSET PEAK DURATION
E
PO unknown several weeks 6wk†
Contraindicated in: Hypersensitivity to donepezil or piperidine derivatives.
Use Cautiously in: Underlying cardiac disease, especially sick sinus syndrome or supraventricular conduction defects; History of ulcer disease
or currently taking
NSAIDs; History of seizures; History of asthma or obstructive pulmonary disease; OB, Lactation, Pedi: Safety note stablished; assumed to be
secreted in breastmilk. Discontinue drug or bottle-feed.
CNS: headache, abnormal dreams, depression, dizziness, drowsiness, fatigue, insomnia, syncope, sedation (unusual). CV: atrial fibrillation,
hypertension, hypotension, vasodilation. GI: diarrhea, nausea, anorexia, vomiting, weight gain (unusual). GU: frequent urination.
Derm:ecchymoses. Metab: hot flashes, weight loss. MS: arthritis, muscle cramps.
Interactions
Drug-Drug: Exaggerates muscle relaxation from succinyl choline. Interferes with the action of anticholinergics. Increase cholinergic effects of
bethanechol. May increase risk of GI bleeding from NSAIDs. Quinidine and ketoconazole decrease metabolism of donepezil. Rifampin,
carbamazepine, dexamethasone, phenobarbital, and phenytoin induce the enzymes that metabolize donepezil and may pits effects.
Drug-Natural Products: Jimson weed and scopolia may antagonize cholinergic effects.
Route/Dosage
Mild to Moderate Alzheimer’s Disease
PO (Adults): 5mg once daily; after 4–6wk may increase to 10mg once daily (dose should not exceed 5mg/day in frail, elderly females).
Severe Alzheimer’s Disease
PO(Adults): 5mg once daily; may increase to 10mg once daily after4–6wk; after 3mo, may then increase to 23mg once daily.
NURSINGIMPLICATIONS
Assessment
● Assess cognitive function (memory, attention, reasoning, language, ability to perform simple tasks) periodically during therapy.
● Monitor heart rate periodically during therapy. May cause bradycardia.
Disturbed thought process (Indications)
Impaired environmental interpretation syndrome (Indications)
Risk for injury (Indications)
Implementation
● Do not confuse Aricept with Aciphex or Azilect.
● PO: Administer in the evening just before going to bed. May be taken without regard to food.
● Oral disintegrating tablets should be allowed to dissolve on tongue; follow with water.
● Swallow 23 mg tablet whole. Do not split, crush or chew; may increase rate of absorption.
● Emphasize the importance of taking donepezil daily, as directed. Missed doses should be skipped and regular schedule returned to the
following day. Do not take more than prescribed; higher doses do not increase effects but may increase side effects.
● Inform patient/family that it may take weeks before improvement in baseline behavior is observed.
● Caution patient and caregiver that donepezil may cause dizziness.
● Advise patient and caregiver to notify health care professional if nausea, vomiting, diarrhea, or changes in color of stool occur or if new
symptoms occur or previously noted symptoms increase in severity.
● Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult
health care professional before taking other Rx, OTC, or herbal products.
● Advise patient and caregiver to notify health care professional of medication regimen before treatment or surgery.
● Emphasize the importance of follow-up exams to monitor progress. Evaluation/Desired Outcomes
● Improvement in cognitive function (memory, attention, reasoning, language, ability to perform simple tasks) in patients with Alzheimer’s
disease
ADRENERGIC DRUGS AFFECTING THE AUTONOMIC NERVOUS SYSTEM

A. Adrenergic drugs
Adrenergic drugs are medications that stimulate certain nerves in your body. They do this either by mimicking the action of the chemical
messengers' epinephrine and norepinephrine or by stimulating their release. These drugs are used in many life-threatening conditions,
including cardiac arrest, shock, asthma attack, or allergic reaction.
1. Phenylephrine (fen-il-eff-rin)
Neo-Synephrine
Classification
Therapeutic: vasopressors
Pharmacologic:adrenergics, alpha adrenergic agonists, vasopressors
Pregnancy Category B, C (Ophth, Parenteral)
Indications
Management of hypotension associated with shock that may persist after adequate fluid replacement.
Management of hypotension associated with anesthesia. Anesthesia adjunct: Prolongation of the
duration of spinal anesthesia. Localization of the effect of regional anesthesia.
Action
Constricts blood vessels by stimulating alpha-adrenergic receptors.
Therapeutic Effects: Increased BP.
Pharmacokinetics
Absorption: Well absorbed from IM sites.
Distribution: Unknown.
Metabolism and Excretion: Metabolized by the liver and other tissues.
Half-life: 2.5 hr.
TIME/ACTION PROFILE (vasopressor effects)
ROUTE ONSET PEAK DURATION
IV Immediate Unknown 10-15 min
IM 10-15 min Unknown 0.5-2 hr
Subcut 10-15 min unknown 50-60 min
Contraindicated in: Uncorrected fluid volume deficits; Tachyarrhythmias; Pheochromocytoma; Angle-closure glaucoma; Acute pancreatitis;
Hepatitis; Hypersensitivity to bisulfites.
Use Cautiously in: Occlusive vascular diseases; Cardiovascular disease; Diabetes mellitus; OB, Lactation: Safety not established. Exercise
Extreme Caution in: Geri: More likely to experience adverse reactions, which result in hallucinations, convulsions, CNS depression, and death;
Hyperthyroidism; Bradycardia; Partial heart block; Severe cardiovascular disease.
CNS: anxiety dizziness, headache, insomnia, nervousness, restlessness, trembling, weakness. Resp: dyspnea, respiratory distress. CV:
ARRHYTHMIAS, bradycardia, chest pain, hypertension, tachycardia, vasoconstriction. Derm: blanching, pallor, piloerection, sweating.
Local: phlebitis, sloughing at IV sites. Neuro: tremor.
Interactions
Drug-Drug: Use with general anesthetics may result in myocardial irritability; use with extreme caution. Use with MAO inhibitors, ergot
alkaloids (ergonovine, methylergonovine), or oxytocics results in severe hypertension. Alpha-adrenergic blockers (phentolamine) may
antagonize vasopressor effects. Atropine blocks bradycardia from phenylephrine and enhances pressor effects.
Route/Dosage
Hypotension
Subcut, IM (Adults): 2– 5 mg.
Subcut, IM (Children): 0.1 mg/kg/dose q 1– 2 hr as needed, maximum dose 5 mg.
IV (Adults): 0.2 mg (range 0.1– 0.5 mg), may be repeated q 10– 15 min or as an infusion at 100– 180 mcg/min initially, 40– 60 mcg/min
maintenance.
IV (Children): 5– 20 mcg/kg/dose q 10– 15 min as needed or 0.1– 0.5 mcg/kg/ min infusion, titrate to effect.
Hypotension during Spinal Anesthesia
Subcut, IM (Adults): 2– 3 mg has been used 3– 4 min before spinal anesthesia to prevent hypotension. IM, Subcut (Children): — 0.5– 1
mg/25 lb body weight.
IV (Adults): 0.2 mg; may repeat q 10– 15 min and may be increase by 0.1– 0.2 mg/dose (not to exceed 0.5 mg/dose).
Vasoconstrictor for Regional Anesthesia
Local (Adults): Add 1 mg to every 20 mL of local anesthetic (yields a 1:20,000 solution).
Prolongation of Spinal Anesthesia
Spinal(Adults): 2– 5 mg added to anesthetic solution.
Assessment
● Monitor BP every 2– 3 min until stabilized and every 5 min thereafter during IV administration.
● Monitor ECG continuously for arrhythmias during IV administration.
● Assess IV site frequently throughout infusion. Antecubital or other large vein should be used to minimize risk of extravasation, which may
cause tissue necrosis. If extravasation occurs, the site should be infiltrated promptly with 10– 15 mL of 0.9% NaCl solution containing 5– 10
mg of phentolamine to prevent necrosis and sloughing.
Decreased cardiac output (Indications)
Ineffective tissue perfusion (Indications)
Implementation
● High Alert: Patient harm and fatalities have occurred from medication errors with phenylephrine. Prior to administration, have second
practitioner independently check original order, dose calculations, concentration, route of administration and infusion pump settings.
IV Administration
● IV: Blood volume depletion should be corrected, if possible, before initiation of IV phenylephrine.
● Direct IV: Diluent: Dilute each 1 mg with 9 mL of sterile water for injection. Rate: Administer each single dose over 1 min.
● Continuous Infusion: Diluent: Dilute 10 mg in 250 or 500 mL of dextrose/ Ringer’s or lactated Ringer’s combination, dextrose/saline
combinations, D5W, D10W, Ringer’s or LR, 0.45% NaCl, or 0.9% NaCl. Concentration: 125,000 or 150,000 solution, respectively. Rate:
Titrate rate according to patient response. Infuse via infusion pump to ensure accurate dose rate.
● Y-Site Compatibility: alfentanil, amikacin, aminophylline, amiodarone, amphotericin B liposome, anidulafungin, argatroban, ascorbic acid,
atropine, aztreonam, benztropine, bivalirudin, bleomycin, bumetanide, buprenorphine, butorphanol, calcium chloride, calcium gluconate,
carboplatin, carmustine, caspofungin, cefazolin, cefonocid, cefoperazone, cefotaxime, cefotetan, cefoxitin, ceftazidime, cephalothin,
chloramphenicol, cisatracurium, cisplatin, clindamycin, cyanocobalamin, cyclophosphamide, cyclosporine, cytarabine, dactinomycin,
daptomycin, dexamethasone, dexmedetomidine, digoxin, diltiazem, diphenhydramine, dobutamine, docetaxel, dopamine, doripenem,
doxorubicin hydrochloride, doxycycline, enalaprilat, ephedrine, epinephrine, epirubicin, epoetin alfa, eptifibatide, ertapenem, erythromycin,
esmolol, etomidate, etoposide, etoposide phosphate, famotidine, fenoldopam, fentanyl, fluconazole, fludarabine, fluorouracil, folic acid,
gentamicin, glycopyrrolate, granisetron, heparin, hetastarch, hydrocortisone, hydromorphone, idarubicin, ifosfamide, imipenem/ cilastatin,
irinotecan, isoproterenol, ketorolac, labetalol, levofloxacin, lidocaine, linezolid, lorazepam, magnesium sulfate, mannitol, mechlorethamine,
meperidine, methotraxate, methoxamine, methyldopate, methtylprednisolone, metoclopramide, metoprolol, metronidazole, micafungin,
miconazole, midazolam, milrinone, mitoxantrone, morphine, multivitamins, mycophenolate, nafcillin, nalbuphine, naloxone, nitroglycerin,
nitroprusside, norepinephrine, octreotide, ondansetron, oxacillin, oxaliplatin, oxytocin, paclitaxel, palonsetron, pantoprazole, papaverine,
penicillin G , pentobarbi1tol, phenobarbitol, phentolamine, phytonadione, piperacillin/tazobactam, potassium acetate, potassium chloride,
procainamide, prochlorperazine, promethazine, propranolol, protamine, pyridoxime, quinupristin/dalfopristin, ranitidine, remifentanil,
rocuronium, sodium acetate, sodium bicarbonate, streptokinase, succinylcholine, sufentanil, tacrolimus, telavancin, teniposide, theophylline,
thiamine, thiotepa, ticarcillin/clavulanate, tigecycline, tirofiban, tobramycin, tolazoline, vancomycin, vasopressin, vecuronium, verapamil,
vincristine, vinorelbine, voriconazole, zidovudine, zoledronic acid. ● Y-Site Incompatibility: acyclovir, amphotericin B colloidal, azathioprine,
dantrolene, diazepam, diazoxide, furosemide, ganciclovir, indomethacin, insulin, pentamidine, phenytoin, trimethoprim/sulfamethoxazole,
thiopental.
● Anesthesia: Phenylephrine 2– 5 mg may be added to spinal anesthetic solution to prolong anesthesia.
● Phenylephrine 1 mg may be added to each 20 mL of local anesthetic to produce vasoconstriction. Patient/Family Teaching
● IV: Instruct patient to report headache, dizziness, dyspnea, or pain at IV infusion site promptly. Evaluation/Desired Outcomes
● Increase in BP to normal range.
● Prolonged duration of spinal anesthesia.
● Localization of regional anesthesia
2. Prazosin (pra-zoe-sin)
Minipress
Classification
Therapeutic: anti-hypertensives
Pharmacologic: peripherally acting anti-adrenergics
Indications
Mild to moderate hypertension. Unlabeled Use: Management of urinary outflow obstruction in patients
with benign prostatic hyperplasia.
Action
Dilates both arteries and veins by blocking postsynaptic alpha1-adrenergic receptors. Decreases
contractions in smooth muscle of prostatic capsule.
Therapeutic Effects: Lowering of BP. Decreased cardiac preload and afterload. Decreased symptoms of
prostatic hyperplasia (urinary urgency, urinary hesitancy, nocturia).
Pharmacokinetics
Absorption: 60% absorbed following oral administration.
Distribution: Widely distributed. Protein Binding: 97%.
Metabolism and Excretion: Extensively metabolized by the liver. Minimal (5– 10%) renal excretion of unchanged drug.
Half-life: 2– 3 hr
TIME/ACTION PROFILE (antihypertensive effects)
ROUTE ONSET PEAK DURATION
PO 2 hr 2–4 hr† 10 hr
†Following single dose; maximal antihypertensive effects occur after 3–4 wk of chronic dosing
Contraindicated in: Hypersensitivity.
Use Cautiously in: Renal insufficiency (increase sensitivity to effects; dose decrease may be required); OB, Lactation, Pedi: Safety not
established; Angina pectoris; When adding diuretics (increase dose of prazosin); Patients undergoing cataract surgery (decrease risk of
intraoperative floppy iris syndrome). Adverse Reactions/Side Effects
CNS: dizziness, headache, weakness, drowsiness, mental depression, syncope. EENT: blurred vision, intraoperative floppy iris syndrome.
CV: first-dose orthostatic hypotension, palpitations, angina, edema. GI: abdominal cramps, diarrhea, dry mouth, nausea, vomiting. GU:
erectile dysfunction, priapism.
Interactions
Drug-Drug: Additive hypotension with acute ingestion of alcohol, other anti-hypertensives, or nitrates. Antihypertensive effects may be
decrease by NSAIDs.
Route/Dosage
Hypertension
PO (Adults): 1 mg 2– 3 times daily (give first dose at bedtime) for initial 3 days of therapy, then increase gradually to maintenance dose of 6–
15 mg/day in 2– 3 divided doses (not to exceed 20– 40 mg/day).
PO (Children): 50– 400 mcg (0.05– 0.4 mg)/kg/day in 2– 3 divided doses (not to exceed 7 mg/dose or 15 mg/day).
Benign Prostatic Hyperplasia
PO (Adults): 1– 5 mg twice daily.
Assessment
● Assess for first-dose orthostatic reaction (dizziness, weakness) and syncope. May occur 30 min– 2 hr after initial dose and occasionally
thereafter. Incidence may be dose related. Volume-depleted or sodium-restricted patients may be more sensitive. Observe patient closely
during this period; take precautions to prevent injury. First dose may be given at bedtime to minimize this reaction.
● Monitor intake and output ratios and daily weight; assess for edema daily, especially at beginning of therapy.
● Hypertension: Monitor BP and pulse frequently during initial dosage adjustment and periodically throughout therapy. Report significant
changes.
● Monitor frequency of prescription refills to determine adherence.
● Benign Prostatic Hyperplasia: Assess patient for symptoms of prostatic hyperplasia (urinary hesitancy, feeling of incomplete bladder
emptying, interruption of urinary stream, impairment of size and force of urinary stream, terminal urinary dribbling, straining to start flow,
dysuria, urgency) before and periodically during therapy.
● Rule out prostatic carcinoma before therapy; symptoms are similar.
Risk for injury (Side Effects)
Noncompliance (Patient/Family Teaching)
Implementation
● May be used in combination with diuretics or beta blockers to minimize sodium and water retention. If these are added to prazosin therapy,
reduce dose of prazosin initially and titrate to effect.
● PO: Administer daily dose at bedtime. If necessary, dose may be increased to twice daily. Patient/Family
Teaching
● Instruct patient to take medication at the same time each day. Take missed doses as soon as remembered. If not remembered until next day,
omit; do not double doses.
● Advise patient to weigh self twice weekly and assess feet and ankles for fluid retention.
● May cause dizziness or drowsiness. Advise patient to avoid driving or other activities requiring alertness until response to the medication is
known.
● Caution patient to avoid sudden changes in position to decrease orthostatic hypotension. Alcohol, CNS depressants, standing for long
periods, hot showers, and exercising in hot weather should be avoided because of enhanced orthostatic effects.
● Advise patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult with
health care professional before taking other medications, especially cough, cold, or allergy remedies.
● Instruct patient to notify health care professional of medication regimen before any surgery.
● Advise patient to notify health care professional if frequent dizziness, fainting, or swelling of feet or lower legs occurs.
● Emphasize the importance of follow-up exams to evaluate effectiveness of medication.
● Hypertension: Emphasize the importance of continuing to take this medication as directed, even if feeling well. Medication controls but does
not cure hypertension.
● Encourage patient to comply with additional interventions for hypertension (weight reduction, low-sodium diet, smoking cessation,
moderation of alcohol consumption, regular exercise, and stress management).
● Instruct patient and family on proper technique for BP monitoring. Advise them to check BP at least weekly and to report significant
changes.
Evaluation/Desired Outcomes
● Decrease in BP without appearance of side effects.
● Decrease in symptoms of prostatic hyperplasia.
Drug Name
Generic Name: atenolol
Brand Name: Apo-Atenolol (CAN), Gen-Atenolol (CAN), Novo-Atenol (CAN), Tenormin
Classification: Beta1-selective adrenergic blocker, Antianginal, Antihypertensive
Pregnancy Category D
Dosage & Route
 Available forms: Tablets—25, 50, 100 mg; injection—5 mg/10 mL
ADULTS
 Hypertension: Initially, 50 mg PO once a day; after 1–2 wk, dose may be increased to 100 mg/day.
 Angina pectoris: Initially, 50 mg PO daily. If optimal response is not achieved in 1 wk, increase to 100
mg daily; up to 200 mg/day may be needed.
 Acute MI: Initially, 5 mg IV given over 5 min as soon as possible after diagnosis; follow with IV injection of 5 mg 10 min later. Switch to 50 mg
PO 10 min after the last IV dose; follow with 50 mg PO 12 hr later. Thereafter, administer 100 mg PO daily or 50 mg PO bid for 6–9 days or until
discharge from the hospital.
PEDIATRIC PATIENTS
 Safety and efficacy not established.
Therapeutic actions
 Blocks beta-adrenergic receptors of the sympathetic nervous system in the heart and juxtaglomerular apparatus (kidney), thus decreasing the
excitability of the heart, decreasing cardiac output and oxygen consumption, decreasing the release of renin from the kidney, and lowering BP.
Indications
 Treatment of angina pectoris due to coronary atherosclerosis
 Hypertension, as a step 1 agent, alone or with other drugs, especially diuretics
 Treatment of MI
 Unlabeled uses: Prevention of migraine headaches; alcohol withdrawal syndrome, treatment of ventricular and supraventricular arrhythmias
Adverse effects
 Allergic reactions: Pharyngitis, erythematous rash, fever, sore throat, laryngospasm,respiratory distress
 CNS: Dizziness, vertigo, tinnitus, fatigue, emotional depression, paresthesias, sleep disturbances, hallucinations, disorientation, memory loss,
slurred speech
 CV: Bradycardia, CHF, cardiac arrhythmias, sinoatrial or AV nodal block, tachycardia, peripheral vascular insufficiency, claudication, CVA,
pulmonary edema, hypotension
 Dermatologic: Rash, pruritus, sweating, dry skin
 EENT: Eye irritation, dry eyes, conjunctivitis, blurred vision
 GI: Gastric pain, flatulence, constipation, diarrhea, nausea, vomiting, anorexia, ischemic colitis, renal and mesenteric arterial thrombosis,
retroperitoneal fibrosis, hepatomegaly, acute pancreatitis
 GU: Impotence, decreased libido, Peyronie’s disease, dysuria, nocturia, frequent urination
 Musculoskeletal: Joint pain, arthralgia, muscle cramps
 Respiratory: Bronchospasm, dyspnea, cough, bronchial obstruction, nasal stuffiness, rhinitis, pharyngitis (less likely than with propranolol)
 Other: Decreased exercise tolerance, development of antinuclear antibodies, hyperglycemia or hypoglycemia, elevated serum transaminase,
alkaline phosphatase, and LDH
Contraindications
 Contraindicated with sinus bradycardia, second- or third-degree heart block, cardiogenic shock, CHF, pregnancy.
 Use cautiously with renal failure, diabetes or thyrotoxicosis (atenolol can mask the usual cardiac signs of hypoglycemia and thyrotoxicosis),
lactation, respiratory disease.
Nursing considerations
Interventions
 WARNING: Do not discontinue drug abruptly after long-term therapy (hypersensitivity to catecholamines may have developed, causing
exacerbation of angina, MI, and ventricular arrhythmias). Taper drug gradually over 2 wk with monitoring.
 Consult physician about withdrawing drug if patient is to undergo surgery (withdrawal is controversial).
Teaching points
 Take drug with meals if GI upset occurs.
 Do not stop taking this drug unless told to do so by a health care provider.
 Avoid driving or dangerous activities if dizziness or weakness occurs.
 You may experience these side effects: Dizziness, light-headedness, loss of appetite, nightmares, depression, sexual impotence.
 Report difficulty breathing, night cough, swelling of extremities, slow pulse, confusion, depression, rash, fever, sore throat.
Drug Name
Generic Name : carvedilol
Brand Name: Coreg
Classification: Alpha- and beta-adrenergic blocker, Antihypertensive
Dosage & Route
Oral
 hypertension
 Adult: Initially, 12.5 mg once daily increased to 25 mg once daily after 2 days. Alternatively, initial dose of 6.25 mg bid increased to 12.5
mg bid after 1-2 wk, increased further if necessary to 50 mg once daily or in divided doses.
 Elderly: 12.5 mg once daily.
 Angina pectoris
 Adult: Initially, 12.5 mg bid increased to 25 mg bid after 2 days.
 heart failure
 Adult: Initially, 3.125 mg bid, doubled to 6.25 mg bid after 2 wk if tolerated, then gradually increased to the max dose the patient can
tolerate at intervals of not <2 wk. Max dose: >85 kg: 50 mg bid; <85 kg: 25 mg bid.
 Left ventricular dysfunction post myocardial infarction
 Adult: Initially: 6.25 mg bid, if tolerated, after 3-10 days, increase to 12.5 mg bid and then to a target dose of 25 mg bid.
Therapeutic actions
 Carvedilol causes vasodilation by blocking the activity of α-blockers, mainly at alpha-1 receptors. It exerts antihypertensive effect partly by
reducing total peripheral resistance and vasodilation. It is used in patients with renal impairment, NIDDM or IDDM.
 Absorption: Absorbed well from the GI tract (oral); peak plasma concentrations after 1-2 hr.
 Distribution: Enters breast milk. Protein-binding: >98%.
 Metabolism: Hepatic: Considerable first-pass effect.
 Excretion: Via bile (as metabolites); 6-10 hr (elimination half-life).
Indications
 Hypertension, alone or with other oral drugs, especially diuretics
 Treatment of mild to severe CHF of ischemic or cardiomyopathic origin with digitalis, diuretics, ACE inhibitors
 Left ventricular dysfunction (LVD) after MI
 Unlabeled uses: Angina (25–50 mg bid)
Adverse effects
 Bradycardia, AV block, angina pectoris, hypervolemia, leucopenia, hypotension, peripheral edema, allergy, malaise, fluid overload, melena,
periodontitis, hyperuricemia, hyponatremia, increased alkaline phosphatase, glycosuria, prothrombin time, SGPT and SGOT levels, purpura,
somnolence, impotence, albuminuria, hypokinesia, nervousness, sleep disorder, skin reaction, tinnitus, dry mouth, anemia, sweating, fatigue,
arthralgia, aggravation, dizziness. Diarrhea, nausea, vomiting, insomnia, hypercholesterolemia, weight gain, abnormal vision, rhinitis, pharyngitis
and hypertriglyceridemia.
Contraindications
 Hypersensitivity; severe chronic heart failure, bronchial asthma or related bronchospastic conditions; severe hepatic impairment. Patients with
NYHA class IV cardiac failure, 2nd or 3rd ° AV block, sick sinus syndrome (unless a permanent pacemaker is in place), cardiogenic shock or
severe bradycardia. Lactation.
Interventions
 WARNING: Do not discontinue drug abruptly after chronic therapy (hypersensitivity to catecholamines may have developed, causing exacerbation
of angina, MI, and ventricular arrhythmias); taper drug gradually over 2 wk with monitoring.
 Consult with physician about withdrawing drug if patient is to undergo surgery (withdrawal is controversial).
 Give with food to decrease orthostatic hypotension and adverse effects.
 Monitor for orthostatic hypotension and provide safety precautions.
 Monitor diabetic patient closely; drug may mask hypoglycemia or worsen hyperglycemia.
 WARNING: Monitor patient for any sign of hepatic impairment (pruritus, dark urine or stools, anorexia, jaundice, pain); arrange for LFTs and
discontinue drug if tests indicate liver injury. Do not restart carvedilol.
Teaching points
 Take drug with meals.
 Do not stop taking drug unless instructed to do so by a health care provider.
 Avoid use of over-the-counter medications.
 Advise the diabetic patient to promptly report changes in glucose.
 You may experience these side effects: Depression, dizziness, light-headedness (avoid driving or performing dangerous activities; getting up and
changing positions slowly may help ease dizziness).
 Report difficulty breathing, swelling of extremities, changes in color of stool or urine, very slow heart rate, continued dizziness.
Drug name
Generic Name: alprazolam
Brand Name: Alprazolam Intensol, Apo-Alpraz (CAN), Niravam, Novo-Alprazol (CAN), Nu-Alpraz
(CAN), Xanax, Xanax TS (CAN), Xanax XR
Classification: Benzodiazepine, Anxiolytic
Pregnancy Category D
Controlled Substance C-IV
Dosages
 Individualize dosage; increase dosage gradually to avoid adverse effects.
ADULTS
 Anxiety disorders: Initially, 0.25–0.5 mg PO tid; adjust to maximum daily dose of 4 mg/day in divided doses or extended-release form once per day
in the AM once dosage is established (immediate release, intensol solution).
 Panic disorder: Initially, 0.5 mg PO tid; increase dose at 3- to 4-day intervals in increments of no more than 1 mg/day; ranges of 1–10 mg/day have
been needed; extended-release form once per day in AM once dosage is established (Xanax products, Niravam).
UNLABELED USES
 Social phobia: 2–8 mg/day PO.
 PMS: 0.25 mg PO tid.
Therapeutic actions
 Exact mechanisms of action not understood; main sites of action may be the limbic system and reticular formation; increases the effects of GABA,
an inhibitory neurotransmitter; anxiety blocking effects occur at doses well below those necessary to cause sedation, ataxia.
Indications
 Management of anxiety disorders, short-term relief of symptoms of anxiety; anxiety associated with depression.
 Treatment of panic attacks with or without agoraphobia
 Unlabeled uses: Social phobia, premenstrual syndrome, depression
Adverse effects
 CNS: Transient, mild drowsiness initially; sedation, depression, lethargy, apathy, fatigue, light-headedness, disorientation, anger, hostility, episodes
of mania and hypomania, restlessness, confusion, crying, delirium, headache, slurred speech, dysarthria, stupor, rigidity, tremor, dystonia, vertigo,
euphoria, nervousness, difficulty in concentration, vivid dreams, psychomotor retardation, extrapyramidal symptoms; mild paradoxical excitatory
reactions during first 2 wk of treatment
 CV: Bradycardia, tachycardia, CV collapse, hypertension, hypotension, palpitations, edema
 Dermatologic: Urticaria, pruritus, rash, dermatitis
 EENT: Visual and auditory disturbances, diplopia, nystagmus, depressed hearing, nasal congestion
 GI: Constipation, diarrhea, dry mouth, salivation, nausea, anorexia, vomiting, difficulty in swallowing, gastric disorders, hepatic impairment
 GU: Incontinence, changes in libido, urinary retention, menstrual irregularities
 Hematologic: Elevations of blood enzymes—LDH, alkaline phosphatase, AST, ALT; blood dyscrasias—agranulocytosis, leukopenia
 Other: Hiccups, fever, diaphoresis, paresthesias, muscular disturbances, gynecomastia. Drug dependence with withdrawal syndrome when drug is
discontinued; more common with abrupt discontinuation of higher dosage used for longer than 4 mo
Contraindications
 Contraindicated with hypersensitivity to benzodiazepines, psychoses, acute narrow-angle glaucoma, shock, coma, acute alcoholic intoxication with
depression of vital signs, pregnancy (crosses the placenta; risk of congenital malformations, neonatal withdrawal syndrome), labor and delivery
(“floppy infant” syndrome), lactation (secreted in breast milk; infants become lethargic and lose weight).
 Use cautiously with impaired liver or kidney function, debilitation.
CLINICAL ALERT! Name confusion has occurred among Xanax (alprazolam), Celexa (citalopram), and Cerebyx (fosphenytoin), and between alprazolam
and lorazepam; use caution.
Interventions
 Arrange to taper dosage gradually after long-term therapy, especially in epileptic patients.
 Do not administer with grapefruit juice.
 Taper drug slowly; decrease by no more than 0.5 mg every 3 days.
Teaching points
 Take this drug exactly as prescribed; take extended-release form once a day in the morning; place rapidly disintegrating tablet on top of tongue,
where it will disintegrate and can be swallowed with saliva.
 Do not drink grapefruit juice while on this drug.
 Do not stop taking drug (in long-term therapy) without consulting health care provider; drug should not be stopped suddenly.
 Avoid alcohol, sleep-inducing, or over-the-counter drugs.
 You may experience these side effects: Drowsiness, dizziness (these effects will be less pronounced after a few days, avoid driving a car or
engaging in other dangerous activities if these occur); GI upset (take drug with food); fatigue; depression; dreams; crying; nervousness.
 Report severe dizziness, weakness, drowsiness that persists, rash or skin lesions, difficulty voiding, palpitations, swelling in the extremities.
Drug Name
Generic Name : clonazepam
Brand Name: Apo-Clonazepam (CAN), Gen-Clonazepam (CAN), Klonopin, Klonopin Wafers, Nu-
Clonazepam (CAN), Rivotril (CAN)
Classification: Benzodiazepine, Antiepileptic
Pregnancy Category X
Controlled Substance C-IV
Dosage & Route
 Individualize dosage; increase dosage gradually to avoid adverse effects; drug is available only in oral dosage forms.
Adults
 Seizure disorders: Initial dose should not exceed 1.5 mg/day PO divided into three doses; increase in increments of 0.5–1 mg PO every 3 days until
seizures are adequately controlled or until side effects preclude further increases. Maximum recommended dosage is 20 mg/day.
 Panic disorders: Initial dose 0.25 mg PO bid; gradually increase to a target dose of 1 mg/day.
Pediatric Patients> 10 YR OR 30 KG
 Initially, 0.01–0.03 mg/kg/day PO; do not exceed 0.05 mg/kg/day PO, given in two or three doses. Increase dosage by not more than 0.25–0.5 mg
every third day until a daily maintenance dose of 0.1–0.2 mg/kg has been reached, unless seizures are controlled by lower dosage or side effects
preclude increases. Whenever possible, divide daily dose into three equal doses, or give largest dose at bedtime.
Therapeutic actions
 Clonazepam is an effective anticonvulsant. It raises the threshold for propagation of seizure activity and prevents generalization of focal or local
activity. Clinically, it improves focal epilepsy and generalized seizures. It is also believed to enhance the activity of GABA, and acts as anxiolytic.
Indications
 Used alone or as adjunct in treatment of Lennox-Gastaut syndrome (petit mal variant), akinetic and myoclonic seizures; may be useful in patients
with absence (petit mal) seizures who have not responded to succinimides; up to 30% of patients show loss of effectiveness of drug, often within 3
mo of therapy (may respond to dosage adjustment); treatment of panic disorder with or without agoraphobia
 Unlabeled uses: Periodic leg movements during sleep; hypokinetic dysarthria, acute manic episodes, multifocal tic disorders, neuralgias
Adverse effects
 Drowsiness, fatigue, muscular hypotonia, coordination disturbances, dizziness, vertigo, anorexia, visual disturbances, libido changes.
 Potentially Fatal: Salivary or bronchial hypersecretion leading to respiratory problems (children). May produce diminished reflexes or coma.
Rarely, blood dyscrasias.
Contraindications
 Hypersensitivity to benzodiazepines, acute pulmonary insufficiency, acute narrow angle glaucoma.
CLINICAL ALERT! Name confusion has occurred between Klonopin (clonazepam) and clonidine; use caution.
Interventions
 Monitor addiction-prone patients carefully because of their predisposition to habituation and drug dependence.
 Monitor liver function and blood counts periodically in patients on long-term therapy.
 WARNING: Taper dosage gradually after long-term therapy, especially in patients with epilepsy; substitute another antiepileptic.
 Monitor patient for therapeutic drug levels: 20–80 ng/mL.
 If the patient has epilepsy, arrange for patient to wear medical alert identification indicating patient has epilepsy and is receiving drug therapy.
Teaching points
 Take drug exactly as prescribed; do not stop taking drug (long-term therapy) without consulting health care provider.
 Avoid alcohol, sleep-inducing, or over-the-counter drugs.
 Avoid pregnancy; serious adverse effects can occur. Using barrier contraceptives is advised while taking this drug.
 It would be advisable to wear or carry a medical alert identification indicating your diagnosis and drug therapy.
 You may experience these side effects: Drowsiness, dizziness (may become less pronounced; avoid driving or engaging in other dangerous
activities); GI upset (take drug with food); fatigue; dreams; crying; nervousness; depression, emotional changes; bed-wetting, urinary incontinence.
 Report severe dizziness, weakness, drowsiness that persists, rash or skin lesions, difficulty voiding, palpitations, swelling in the extremities.
Drug Name
Generic Name : morphine sulfate
Brand Name:
 Timed-release: Avinza, Kadian, M-Eslon (CAN), MS Contin, Oramorph SR
 Oral solution: Roxanol, Roxanol T
 Rectal suppositories: RMS
 Injection: Astramorph PF, Duramorph
 Preservative-free concentrate for microinfusion devices for intraspinal use: Infumorph
 Liposome injection: DepoDur
Classification: Opioid agonist analgesic
Controlled Substance C-II
Dosage & Route
ADULTS
Oral
 Initial dose, 15 mg PO daily, as a single dose in evening. One-third to one-sixth as effective as parenteral administration because of first-pass
metabolism; 10–30 mg q 4 hr PO. CR: 30 mg q 8–12 ;hr PO or as directed by physician; Kadian: 20–100 mg PO daily–24-hr release system; MS
Contin: 200 mg PO q 12 hr; Avinza: 30 mg PO daily; if opioid naive, increase by 30 mg (or lower) increments q 4 days.
IM or subcutaneous
 10 mg (range, 5–20 mg)/70 kg q 4 hr or as directed by physician.
IV
 2.5–15 mg/70 kg of body weight in 4–5 mL water for injection administered over 4–5 min, or as directed by physician. Continuous IV infusion:
0.1–1 mg/mL in D5W by controlled infusion device.
Rectal
 10–30 mg q 4 hr or as directed by physician.
Epidural
 Initial injection of 5 mg in the lumbar region may provide pain relief for up to 24 hr. If adequate pain relief is not achieved within 1 hr, incremental
doses of 1–2 mg may be given at intervals sufficient to assess effectiveness, up to 10 mg/24 hr. For continuous infusion, initial dose of 2–4 mg/24
hr is recommended. Further doses of 1–2 mg may be given if pain relief is not achieved initially.
Liposome injection
 10–15 mg by lumbar epidural injection using a catheter or needle prior to major surgery or after clamping the umbilical cord during cesarean
section.
Intrathecal
 Dosage is usually one-tenth that of epidural dosage; a single injection of 0.2–1 mg may provide satisfactory pain relief for up to 24 hr. Do not inject
> 2 mL of the 5 mg/10 mL ampule or > 1 mL of the 10 mg/10 mL ampule. Use only in the lumbar area. Repeated intrathecal injections are not
recommended; use other routes if pain recurs. For epidural or intrathecal dosing, use preservative-free morphine preparations only.
PEDIATRIC PATIENTS
 Do not use in premature infants.
IM or subcutaneous
 0.05–0.2 mg/kg (up to 15 mg per dose) q 4 hr or as directed by physician.
GERIATRIC PATIENTS OR IMPAIRED ADULTS
 Use caution. Respiratory depression may occur in the elderly, the very ill, those with respiratory problems. Reduced dosage may be needed.
Epidural
 Use extreme caution; injection of < 5 mg in the lumbar region may provide adequate pain relief for up to 24 hr.
Intrathecal
 Use lower dosages than recommended above for adults.
Therapeutic actions
 Morphine is a phenanthrene derivative which acts mainly on the CNS and smooth muscles. It binds to opiate receptors in the CNS altering pain
perception and response. Analgesia, euphoria and dependence are thought to be due to its action at the mu-1 receptors while respiratory depression
and inhibition of intestinal movements are due to action at the mu-2 receptors. Spinal analgesia is mediated by morphine agonist action at the K
receptor. Cough is suppressed by direct action on cough centre.
Indications
 Relief of moderate to severe acute and chronic pain
 Preoperative medication to sedate and allay apprehension, facilitate induction of anesthesia, and reduce anesthetic dosage
 Analgesic adjunct during anesthesia
 Component of most preparations that are referred to as Brompton’s cocktail or mixture, an oral alcoholic solution that is used for chronic severe
pain, especially in terminal cancer patients
 Intraspinal use with microinfusion devices for the relief of intractable pain
 Treatment of pain following major surgery, ER liposome injection for single-dose administration by epidural route at the lumbar level
Adverse effects
 Convulsions; nausea, vomiting, dry mouth, constipation; urinary retention; headache, vertigo; palpitations; hypothermia; pruritus, urticaria;
tachycardia, bradycardia; blurred vision; miosis; dependency; drowsiness; lightheadedness; dizziness; sweating; dysphoria; euphoria.
 Potentially Fatal: Respiratory depression; circulatory failure; hypotension; deepening coma; anaphylactic reactions.
Contraindications
 Respiratory depression, acute or severe asthma; paralytic ileus; obstructive airway disease; acute liver disease; comatose patients; increased
intracranial pressure; acute alcoholism. Pulmonary oedema resulting from a chemical respiratory irritant.
Interventions
 BLACK BOX WARNING: Caution patient not to chew or crush CR preparations.
 WARNING: Dilute and administer slowly IV to minimize likelihood of adverse effects.
 Tell patient to lie down during IV administration.
 WARNING: Keep opioid antagonist and facilities for assisted or controlled respiration readily available during IV administration.
 WARNING: Use caution when injecting IM or subcutaneously into chilled areas or in patients with hypotension or in shock; impaired perfusion
may delay absorption; with repeated doses, an excessive amount may be absorbed when circulation is restored.
 Reassure patients that they are unlikely to become addicted; most patients who receive opiates for medical reasons do not develop dependence
syndromes.
 BLACK BOX WARNING: Liposome preparation is for lumbar epidural injection only; it should not be given intrathecally, IV, or IM.
Teaching points
 Take this drug exactly as prescribed. Avoid alcohol, antihistamines, sedatives, tranquilizers, and over-the-counter drugs.
 Swallow controlled-release preparation (MS Contin, Oramorph SR) whole; do not cut, crush, or chew.
 Do not take leftover medication for other disorders, and do not let anyone else take your prescription.
 You may experience these side effects: Nausea, loss of appetite (take with food, lie quietly); constipation (use laxative); dizziness, sedation,
drowsiness, impaired visual acuity (avoid driving or performing tasks that require alertness and visual acuity).
 Report severe nausea, vomiting, constipation, shortness of breath or difficulty breathing, rash.
Drug Name
Generic Name : lidocaine hydrochloride ,lidocaine HCl in 5% dextrose , lidocaine HCl without preservatives
Brand Name:
 Antiarrhythmic preparations: Xylocaine HCl IV for Cardiac Arrhythmias
 Local anesthetic preparations: Octocaine, Xylocaine HCl (injectable)
 Topical for mucous membranes: Anestacon, Burn-O-Jel, Dentipatch, DermaFlex, ELA-Max,
Xylocaine, Zilactin-L
 Topical dermatologic: Lidoderm, Numby Stuff, Xylocaine
Classification: Antiarrhythmic, Local anesthetic
Pregnancy Category B
Dosage & Route
ADULTS
IM
 Arrhythmia: Use only the 10% solution for IM injection. 300 mg in deltoid or thigh muscle. Switch to IV lidocaine or oral antiarrhythmic as soon
as possible.
IV bolus
 Arrhythmia: Use only lidocaine injection labeled for IV use and without preservatives or catecholamines. Monitor ECG constantly. Give 50–100
mg at rate of 25–50 mg/min. One-third to one-half the initial dose may be given after 5 min if needed. Do not exceed 200–300 mg in 1 hr.
IV, continuous infusion
 Arrhythmia: Give 1–4 mg/min (or 20–50 mcg/kg/min). Titrate the dose down as soon as the cardiac rhythm stabilizes. Use lower doses in patients
with CHF, liver disease, and in patients > 70 yr.
Topical, intratissue, epidural
 Local anesthesia: Preparations containing preservatives should not be used for spinal or epidural anesthesia. Drug concentration and diluent should
be appropriate to particular local anesthetic use: 5% solution with glucose is used for spinal anesthesia, 1.5% solution with dextrose for low spinal
or “saddle block”; anesthesia. Dosage varies with the area to be anesthetized and the reason for the anesthesia; use the lowest dose possible to
achieve results.
PEDIATRIC PATIENTS
IV
 Arrhythmia: Safety and efficacy have not been established. American Heart Association recommends bolus of 0.5–1 mg/kg IV, followed by 30
mcg/kg/min with caution. The IM auto-injector device is not recommended.
Topical, intratissue, epidural
 Local anesthesia: See adult dosage discussion. Use lower concentrations.
GERIATRIC OR DEBILITATED PATIENTS, PATIENTS WITH LIVER DISEASE OR CHF
 Use lower concentrations in these patients.
Therapeutic actions
 Lidocaine is an amide type local anesthetic. It stabilizes the neuronal membrane and inhibits sodium ion movements, which are necessary for
conduction of impulses. In the heart, lidocaine reduces phase 4 depolarization and automaticity. Duration of action potential and effective refractory
period are also reduced.
Indications
 As antiarrhythmic: Management of acute ventricular arrhythmias during cardiac surgery and MI (IV use). Use IM when IV administration is not
possible or when ECG monitoring is not available and the danger of ventricular arrhythmias is great (single-dose IM use, for example, by
paramedics in a mobile coronary care unit)
 As anesthetic: Infiltration anesthesia, peripheral and sympathetic nerve blocks, central nerve blocks, spinal and caudal anesthesia, retrobulbar and
transtracheal injection; topical anesthetic for skin disorders and accessible mucous membranes
Adverse effects
 Dizziness, paresthesia, drowsiness, confusion, respiratory depression and convulsions.
 Potentially Fatal: Hypotension and bradycardia leading to cardiac arrest; anaphylaxis
Contraindications
 Hypovolemia; heart block or other conduction disturbances.
Interventions
 WARNING: Check drug concentration carefully; many concentrations are available.
 Reduce dosage with hepatic or renal failure.
 Continuously monitor response when used as antiarrhythmic or injected as local anesthetic.
 WARNING: Keep life-support equipment and vasopressors readily available in case severe adverse reaction (CNS, CV, or respiratory) occurs
when lidocaine is injected.
 WARNING: Establish safety precautions if CNS changes occur; have IV diazepam or short-acting barbiturate (thiopental, thiamylal) readily
available in case of seizures.
 WARNING: Monitor for malignant hyperthermia (jaw muscle spasm, rigidity); have life-support equipment and IV dantrolene readily available.
 WARNING: Establish safety precautions if CNS changes occur; have IV diazepam or short-acting barbiturate (thiopental, thiamylal) readily
available in case of seizures.
 WARNING: Monitor for malignant hyperthermia (jaw muscle spasm, rigidity); have life-support equipment and IV dantrolene readily available.
 Titrate dose to minimum needed for cardiac stability, when using lidocaine as antiarrhythmic.
 Reduce dosage when treating arrhythmias in CHF, digitalis toxicity with AV block, and geriatric patients.
 Monitor fluid load carefully; more concentrated solutions can be used to treat arrhythmias in patients on fluid restrictions.
 Have patients who have received lidocaine as a spinal anesthetic remain lying flat for 6–12 hr afterward, and ensure that they are adequately
hydrated to minimize risk of headache.
 WARNING: Check lidocaine preparation carefully; epinephrine is added to solutions of lidocaine to retard the absorption of the local anesthetic
from the injection site. Be sure that such solutions are used only to produce local anesthesia. These solutions should be injected cautiously in body
areas supplied by end arteries and used cautiously in patients with peripheral vascular disease, hypertension, thyrotoxicosis, or diabetes.
 Use caution to prevent choking. Patient may have difficulty swallowing following use of oral topical anesthetic. Do not give food or drink for 1 hr
after use of oral anesthetic.
 Apply lidocaine ointments or creams to a gauze or bandage before applying to the skin.
 WARNING: Monitor for safe and effective serum drug concentrations (antiarrhythmic use: 1–5 mcg/mL). Doses > 6–10 mcg/mL are usually toxic.
Teaching points
 Dosage is changed frequently in response to cardiac rhythm on monitor.
 Oral lidocaine can cause numbness of the tongue, cheeks, and throat. Do not eat or drink for 1 hour after using oral lidocaine to prevent biting the
inside of your mouth or tongue and choking.
 You may experience these side effects: Drowsiness, dizziness, numbness, double vision; nausea, vomiting; stinging, burning, local irritation (local
anesthetic).
 Report difficulty speaking, thick tongue, numbness, tingling, difficulty breathing, pain or numbness at IV site, swelling, or pain at site of local
anesthetic use.
Drug Name
Generic Name: atorvastatin calcium
Brand Name: Lipitor
Classification: Antihyperlipidemic, HMG-CoA reductase inhibitor
Pregnancy Category X
Dosage & Route
ADULTS
 Initially, 10 mg PO once daily without regard to meals; for maintenance, 10–80 mg PO daily.
May be combined with bile acid–binding resin.
PEDIATRIC PATIENTS 10–17 YR
 Initially, 10 mg PO daily. Maximum, 20 mg/day; do not change dose of intervals < 4 wk.
Therapeutic actions
Inhibits HMG-CoA reductase, the enzyme that catalyzes the first step in the cholesterol synthesis pathway, resulting in a decrease in serum cholesterol,
serum LDLs (associated with increased risk of CAD), and increases serum HDLs (associated with decreased risk of CAD); increases hepatic LDL recapture
sites, enhances reuptake and catabolism of LDL; lowers triglyceride levels.
Indications
 Adjunct to diet in treatment of elevated total cholesterol, serum triglycerides, and LDL cholesterol in patients with primary hypercholesterolemia
(types IIa and IIb) and mixed dyslipidemia, primary dysbetalipoproteinemia, and homozygous familial hypercholesterolemia whose response to
dietary restriction of saturated fat and cholesterol and other nonpharmacologic measures has not been adequate
 To increase HDL-C in patients with primary hypercholesterolemia and mixed dyslipidemia
 Adjunct to diet to treat elevated serum triglyceride levels
 Adjunct to diet in treatment of boys and postmenarchal girls ages 10–17 with heterozygous familial cholesterolemia if diet alone is not adequate to
control lipid levels and LDL-C levels are > 190 mg/dL or if LDL-C level is > 160 mg/dL and there is a family history of premature CV disease or
the child has two or more risk factors for the development of coronary disease
 Prevention of CV disease in adults without clinically evident coronary disease but with multiple risk factors for CAD such as age > 55 yr, smoking,
hypertension, low HDL-C, family history of early CAD; to reduce the risk of MI and risk for revascularization procedures and angina
Adverse effects
 CNS: Headache, asthenia
 GI: Flatulence, abdominal pain, cramps, constipation, nausea, dyspepsia, heartburn, liver failure
 Respiratory: Sinusitis, pharyngitis
 Other: Rhabdomyolysis with acute renal failure, arthralgia, myalgia
Contraindications
 Contraindicated with allergy to atorvastatin, fungal byproducts, active liver disease or unexplained and persistent elevations of transaminase levels,
pregnancy, lactation.
 Use cautiously with impaired endocrine function.
CLINICAL ALERT! Name confusion has been reported between written orders for Lipitor (atorvastatin) and Zyrtec (certirizine). Use extreme caution.
Assessment
 History: Allergy to atorvastatin, fungal byproducts; active hepatic disease; acute serious illness; pregnancy, lactation
 Physical: Orientation, affect, muscle strength; liver evaluation, abdominal examination; lipid studies, LFTs, renal function tests
Interventions
 Obtain LFTs as a baseline and periodically during therapy; discontinue drug if AST or ALT levels increase to 3 times normal levels.
 WARNING: Withhold atorvastatin in any acute, serious condition (severe infection, hypotension, major surgery, trauma, severe metabolic or
endocrine disorder, seizures) that may suggest myopathy or serve as risk factor for development of renal failure.
 Ensure that patient has tried cholesterol-lowering diet regimen for 3–6 mo before beginning therapy.
 Administer drug without regard to food, but at same time each day.
 Atorvastatin may be combined with a bile acid–binding agent. Do not combine with other HMG-CoA reductase inhibitors or fibrates.
 Consult dietitian about low-cholesterol diets.
 WARNING: Ensure that patient is not pregnant and has appropriate contraceptives available during therapy; serious fetal damage has been
associated with this drug.
Teaching points
 Take this drug once a day, at about the same time each day, preferably in the evening; may be taken with food. Do not drink grapefruit juice while
taking this drug.
 Institute appropriate dietary changes.
 Arrange to have periodic blood tests while you are taking this drug.
 Alert any health care provider that you are on this drug; it will need to be discontinued if acute injury or illness occurs.
 Do not become pregnant while you are on this drug; use barrier contraceptives. If you wish to become pregnant or think you are pregnant, consult
your health care provider.
 You may experience these side effects: Nausea (eat frequent small meals); headache, muscle and joint aches and pains (may lessen over time).
 Report muscle pain, weakness, tenderness; malaise; fever; changes in color of urine or stool; swelling.
Drug Name
Generic Name : nitroglycerin
Brand Name:
 Intravenous: Generic
 Spray: NitrolingualPumpspray
 Sublingual: Gen-Nitroglycerin (CAN), NitroQuick, Nitrostat
 Sustained-release: Nitro-Time
 Topical: Nitro-Bid
 Transdermal: Deponit, Minitran, Nitrek, Nitro-Dur, Transderm-Nitro
 Translingual: Nitrolingual
 Transmucosal: Nitrogard
Classification: Antianginal, Nitrate
Dosage & Route
Available forms : Injection—0.5, 5 mg/mL; injection solution—25, 50, 100, 200 mg; sublingual tablets—0.3, 0.4, 0.6 mg; translingual spray—0.4
mg/spray; transmucosal tablets—1, 2, 3 mg; transmucosal SR tablets—1, 2, 2.5, 3, 5 mg; oral SR capsules—2.5, 6.5, 9 mg; transdermal—0.1, 0.2, 0.3, 0.4,
0.6, 0.8 mg/hr; topical ointment—2%
ADULTS
IV
 Initial dose, 5 mcg/min delivered through an infusion pump. Increase by 5-mcg/min increments every 3–5 min as needed. If no response at 20
mcg/min, increase increments to 10–20 mcg/min. Once a partial BP response is obtained, reduce dose and lengthen dosage intervals; continually
monitor response and titrate carefully.
Sublingual
 Acute attack: Dissolve 1 tablet under tongue or in buccal pouch at first sign of anginal attack; repeat every 5 min until relief is obtained. Do not
take more than 3 tablets/15 min. If pain continues or increases, patient should call physician or go to hospital.
 Prophylaxis: Use 5–10 min before activities that might precipitate an attack.
SR (oral)
 Initial dose, 2.5–9 mg q 12 hr. Increase to q 8 hr as needed and tolerated. Doses as high as 26 mg given qid have been used.
Topical
 Initial dose, one-half inch q 8 hr. Increase by one-half inch to achieve desired results. Usual dose is 1–2 inches q 8 hr; up to 4–5 inches q 4 hr have
been used. 1 inch = 15 mg nitroglycerin.
Transdermal
 Apply one patch each day. Adjust to higher doses by using patches that deliver more drug or by applying more than one patch. Apply patch to arm;
remove at bedtime.
Translingual
 Spray preparation delivers 0.4 mg/metered dose. At onset of attack, spray one to two metered doses into oral mucosa; no more than three doses/15
min should be used. If pain persists, seek medical attention. May be used prophylactically 5–10 min before activity that might precipitate an attack.
Transmucosal
 1 mg q 3–5 hr during waking hours. Place tablet between lip and gum above incisors, or between cheek and gum.
PEDIATRIC PATIENTS
 Safety and efficacy not established.
Therapeutic actions
 Relaxes vascular smooth muscle with a resultant decrease in venous return and decrease in arterial BP, which reduces left ventricular workload and
decreases myocardial oxygen consumption.
Indications
 Sublingual, translingual preparations: Acute angina
 Oral SR, sublingual, topical, transdermal, translingual, transmucosal preparations: Prophylaxis of angina
 IV: Angina unresponsive to recommended doses of organic nitrates or beta-blockers
 IV: Perioperative hypertension
 IV: CHF associated with acute MI
 IV: To produce controlled hypertension during surgery
 Unlabeled uses: Reduction of cardiac workload in acute MI and in CHF (sublingual, topical); adjunctive treatment of Raynaud’s disease (topical)
Adverse effects
 CNS: Headache, apprehension, restlessness, weakness, vertigo, dizziness, faintness
 CV: Tachycardia, retrosternal discomfort, palpitations, hypotension, syncope, collapse, orthostatic hypotension, angina
 Dermatologic: Rash, exfoliative dermatitis, cutaneous vasodilation with flushing, pallor, perspiration, cold sweat, contact dermatitis—transdermal
preparations, topical allergic reactions—topical nitroglycerin ointment
 GI: Nausea, vomiting, incontinence of urine and feces, abdominal pain
 Local: Local burning sensation at the point of dissolution (sublingual)
 Other: Ethanol intoxication with high-dose IV use (alcohol in diluent)
Contraindications
 Contraindicated with allergy to nitrates, severe anemia, early MI, head trauma, cerebral hemorrhage, hypertrophic cardiomyopathy, pregnancy,
lactation.
 Use cautiously with hepatic or renal disease, hypotension or hypovolemia, increased intracranial pressure, constrictive pericarditis, pericardial
tamponade, low ventricular filling pressure or low PCWP.
CLINICAL ALERT! Name confusion has occurred between NitroBid (nitrogylcerin) and Nicotral (nicotine); between nitroglycerin and nitroprusside; use
caution.
Assessment
 History: Allergy to nitrates, severe anemia, early MI, head trauma, cerebral hemorrhage, hypertrophic cardiomyopathy, hepatic or renal disease,
hypotension or hypovolemia, increased intracranial pressure, constrictive pericarditis, pericardial tamponade, low ventricular filling pressure or low
PCWP, pregnancy, lactation
 Physical: Skin color, T, lesions; orientation, reflexes, affect; P, BP, orthostatic BP, baseline ECG, peripheral perfusion; R, adventitious sounds;
liver evaluation, normal output; LFTs, renal function tests (IV); CBC, Hgb
Interventions
 Give sublingual preparations under the tongue or in the buccal pouch. Encourage patient not to swallow. Ask patient if the tablet “fizzles” or burns.
Always check the expiration date on the bottle; store at room temperature, protected from light. Discard unused drug 6 mo after bottle is opened
(conventional tablets); stabilized tablets (Nitrostat) are less subject to loss of potency.
 Give sustained-release preparations with water; warn the patient not to chew the tablets or capsules; do not crush these preparations.
 Administer topical ointment by applying the ointment over a 6 × 6 inch area in a thin, uniform layer using the applicator. Cover area with plastic
wrap held in place by adhesive tape. Rotate sites of application to decrease the chance of inflammation and sensitization; close tube tightly when
finished.
 Administer transdermal systems to skin site free of hair and not subject to much movement. Shave areas that have a lot of hair. Do not apply to
distal extremities. Change sites slightly to decrease the chance of local irritation and sensitization. Remove transdermal system before attempting
defibrillation or cardioversion. Remove old system before applying a new one.
 Administer transmucosal tablets by placing them between the lip and gum above the incisors or between the cheek and gum. Encourage patient not
to swallow and not to chew the tablet.
 Administer the translingual spray directly onto the oral mucosa; preparation is not to be inhaled.
 WARNING: Arrange to withdraw drug gradually. 4–6 wk is the recommended withdrawal period for the transdermal preparations.
Teaching points
 Place sublingual tablets under your tongue or in your cheek; do not chew or swallow the tablet; the tablet should burn or “fizzle” under the tongue.
Take the nitroglycerin before chest pain begins, when you anticipate that your activities or situation may precipitate an attack. You may repeat your
dose every 5 minutes for a total of three tablets. If the pain is not relieved, go to an emergency room. Do not buy large quantities; this drug does not
store well. Keep the drug in a dark, dry place, in a dark-colored glass bottle with a tight lid; do not combine with other drugs.
 Do not chew or crush the timed-release preparations; take on an empty stomach.
 Spread a thin layer of topical ointment on the skin using the applicator. Do not rub or massage the area. Cover with plastic wrap held in place with
adhesive tape. Wash your hands after application. Keep the tube tightly closed. Rotate the sites frequently to prevent local irritation.
 To use transdermal systems, you may need to shave an area for application. Apply to a slightly different area each day. Remove the old system
before you apply a new one. Use care if changing brands; each system has a different concentration.
 Place transmucosal tablets between the lip and gum or between the gum and cheek. Do not chew; try not to swallow.
 Spray translingual spray directly onto oral mucous membranes; do not inhale. Use 5–10 min before activities that you anticipate will precipitate an
attack.
 You may experience these side effects: Dizziness, light-headedness (may be transient; change positions slowly); headache (lie down in a cool
environment and rest; over-the-counter preparations may not help); flushing of the neck or face (transient).
 Report blurred vision, persistent or severe headache, rash, more frequent or more severe angina attacks, fainting.
Drug Name
Generic Name : heparin , heparin sodium injection, heparin sodium and 0.9% sodium chloride, heparin
sodium lock flush solution
Brand Name: Hepalean (CAN), Heparin Leo (CAN) ,Hepalean-Lok (CAN), Heparin Lock Flush, Hep-
Lock, Hep-Lock U/P
Classification: Anticoagulant
Dosage & Route
Available forms :Injection—1,000, 2,000, 2,500, 5,000, 7,500, 10,000, 12,500, 20,000, 40,000 units/mL;
also single-dose and unit-dose forms; lock flush solution—10, 100 units/mL.
Dosages : Adjust dosage according to coagulation tests. Dosage is adequate when WBCT = 2.5–3 times control—or aPTT = 1.5–2 times control value. The
following are guidelines to dosage:
ADULTS
Subcutaneous (deep subcutaneous injection)
 For general anticoagulation: IV loading dose of 5,000 units and then 10,000–20,000 units subcutaneously followed by 8,000–10,000 units q 8 hr or
15,000–20,000 units q 12 hr.
 Prophylaxis of postoperative thromboembolism: 5,000 units by deep subcutaneous injection 2 hr before surgery and q 8–12 hr thereafter for 7 days
or until patient is fully ambulatory.
IV
 Intermittent IV: Initial dose of 10,000 units and then 5,000–10,000 units q 4–6 hr.
 Continuous IV infusion: Loading dose of 5,000 units and then 20,000–40,000 units/day.
 Surgery of heart and blood vessels for patients undergoing total body perfusion: Not less than 150 units/kg; guideline often used is 300 units/kg for
procedures less than 60 min, 400 units/kg for longer procedures.
 Clot prevention in blood samples: 70–150 units/10–20 mL of whole blood.
 Heparin lock and extracorporeal dialysis: See manufacturer’s instructions.
PEDIATRIC PATIENTS
 Initial IV bolus of 50 units/kg and then 100 units/kg IV q 4 hr, or 20,000 units/m 2 per 24 hr by continuous IV infusion.
Therapeutic actions
 Heparin increases the inhibitory action of antithrombin III (AT III) on clotting factors XIIa, XIa, IXa, Xa and thrombin. This inhibits the conversion
of prothrombin to thrombin and fibrinogen to fibrin. It also inhibits platelet function. It may reduce the activity of ATIII at very high doses.
Indications
 Prevention and treatment of venous thrombosis and pulmonary embolism
 Treatment of atrial fibrillation with embolization
 Diagnosis and treatment of DIC
 Prevention of clotting in blood samples and heparin lock sets and during dialysis procedures
 Unlabeled uses: Adjunct in therapy of coronary occlusion with acute MI, prevention of left ventricular thrombi and CVA post-MI, prevention of
cerebral thrombosis in the evolving CVA
Adverse effects
 Slight fever, headache, chills, nausea, vomiting, constipation, epistaxis, bruising, slight haematuria, skin necrosis (SC inj), osteoporosis, alopecia.
Hypersensitivity reactions include urticaria, conjunctivitis, rhinitis, asthma, angioedema and anaphylactic shock. Priapism.
 Potentially Fatal: Heparin-induced thrombocytopenia with or without thrombosis; bleeding.
Contraindications
 Patients predisposed to active bleeding including thrombocytopenia, peptic ulcer disease, cerebrovascular disorders, haemorrhagic blood disorders,
bacterial endocarditis, severe hypertension, oesophageal varices. Recent surgery at sites where haemorrhage would be an especial risk. Severe renal
and hepatic impairment. Cerebral or subarachnoid haemorrhage, abdominal or thoracic bleeding into closed space, severe traumatic bleed, hepatic,
renal, splenic or arterial injury, severe haemostatic defect, arterial thrombosis with heparin-associated thrombocytopenia. IM admin.
Assessment
 History: Recent surgery or injury; sensitivity to heparin; hyperlipidemia; pregnancy
 Physical: Peripheral perfusion, R, stool guaiac test, PTT or other tests of blood coagulation, platelet count, renal function tests
Interventions
 Adjust dose according to coagulation test results performed just before injection (30 min before each intermittent dose or q 4–6 hr if continuous IV
dose). Therapeutic range aPTT: 1.5–2.5 times control.
 Always check compatibilities with other IV solutions.
 Use heparin lock needle to avoid repeated injections.
 Give deep subcutaneous injections; do not give heparin by IM injection.
 Do not give IM injections to patients on heparin therapy (heparin predisposes to hematoma formation).
 WARNING: Apply pressure to all injection sites after needle is withdrawn; inspect injection sites for signs of hematoma; do not massage injection
sites.
 Mix well when adding heparin to IV infusion.
 Do not add heparin to infusion lines of other drugs, and do not piggyback other drugs into heparin line. If this must be done, ensure drug
compatibility.
 Provide for safety measures (electric razor, soft toothbrush) to prevent injury from bleeding.
 Check for signs of bleeding; monitor blood tests.
 Alert all health care providers of heparin use.
 WARNING: Have protamine sulfate (heparin antidote) readily available in case of overdose; each mg neutralizes 100 units of heparin.
 WARNING: Treatment of overdose: Protamine sulfate (1% solution). Each mg of protamine neutralizes 100 USP heparin units. Give very slowly
IV over 10 min, not to exceed 50 mg. Establish dose based on blood coagulation studies.
Teaching points
 This drug must be given by a parenteral route (cannot be taken orally).
 Frequent blood tests are necessary to determine blood clotting time is within the correct range.
 Be careful to avoid injury: Use an electric razor, avoid contact sports and other activities that might lead to injury.
 You may experience loss of hair.
 Report nose bleed, bleeding of the gums, unusual bruising, black or tarry stools, cloudy or dark urine, abdominal or lower back pain, severe
headache.

Therapeutic: Urinary Tract Stimulants Pharmacologic: Cholinergic

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Therapeutic: Urinary Tract Stimulants Pharmacologic: Cholinergic

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CHOLINERGIC DRUGS AFFECTING AUTONOMIC NERVOUS SYSTEM

ADRENERGIC DRUGS AFFECTING THE AUTONOMIC NERVOUS SYSTEM

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