PREMEDICATION

MODERATOR: DR.DINESH KAUSHAL

PRESENTSD BY: DR RAJESH RAMAN &
DR GOPAL SINGH
 Introduction
Management of anaesthesia begins with preoperative
psychological preparation of the patient and
administration of a drug or drugs selected to elicit
specific pharmacologic responses.

This initial psychological and pharmacologic

component of anaesthetic management before
induction of anaesthesia is referred to as
"Premedication"
 Psychological Premedication is provided by the
anaesthesiologist's preoperative visit and
interview with the patient and family members
The incidence of anxiety is lower in pts visited by
anesthesiologist pre operatively than in those
receiving only pharmacological premedications & no
visit.

 Pharmacological Premedication is administration

of drugs orally/intravenously or intramuscularly
before the anticipated induction of anaesthesia
 Primary Goals for Pharmacologic Premedication

1. Anxiety relief: midazolam, alprazolam,Diazepam, α-2 agonists, barbiturates

2. Sedation:midazolam, alprazolam, Diazepam, α-2 agonists, barbiturates

3. Analgesia: Opioids, NSAIDS

4. Amnesia:midazolam, alprazolam,Diazepam

5. Antisialogogue effect: atropine, glycopyrrolate

6. Antiemesis: ondansetron, metoclopramide, promethazine

7. Increase in gastric fluid pH: ranitidine, pantoprazole, sodium citrate

8. Decreased in gastric fluid volume: metoclopramide, ranitidine

9. Attenuation of sympathetic nervous system reflexes: opioids, β- blockers,α2 agonist

10. Decrease in anesthetic requirements: opiods, benzodiazepines,Alpha-2 agonists

11. Prophylaxis against allergic reactions: avil, promethazine, hydrocortisone

 Secondary Goals for Pharmacologic
Premedication

 Decrease in cardiac vagal activity ...

Anticholinergics (atropine) just before the
time of anticipated need
 Postoperative analgesia ... better
achieved with opioids or the intravenous
injection of an opioids before the painful
stimulus (preemptive analgesia)
 Prevention of postoperative nausea and
vomiting ... intravenous injection of an
antiemetic ( droperidol, ondansetron)
THE 9 A’s OF PREMEDICATION

1. Anxiolytics.
2. Antiemetics.
3. Amnesics.

4. Analgesics
5. Antacids.
6. Anti-autonomic [Symp & parasymp].

7. Antibiotics.
8. Anticoagulants.
9. Antianginal, Antihypertensives, steroids etc.

 1-3 usually used, 4-6 often used, 7-9 occasionally used

 Anxiety:-
 If it is significantly marked, causes all the signs of
sympathetic stimulation & stress: increased H.R.,&
B.P., pale & sweaty skin & venous constriction.
 There may be ventricular ectopic beats& leads to
arrhythmias
 Causes:-
1. Anesthesia
2. Fear of effect of surgery
3. Pre existing illness
4. Leaving the family
5. Nonspecific
The most common worries about
anesthesia are:-
 “Will I be asleep?
 Will I wake up?”

These questions & any about post

operative pain relieve can be answered
by information & reassurance.
 Reducing the Risk for Aspiration
 Certain patients (such as those who are
pregnant, morbidly obese, have hiatal
hernia, or have emotional stress ) are at
greater risk for aspiration
 Drugs used to reduce the risk are:
H2 Receptor Antagonists
Proton pump inhibitors
Metoclopramide
Non particulate/soluble antacids: sodium citrate
Attenuation of sympathetic nervous system reflexes

 Opioids, β-blockers, and α-2 agonists

control blood pressure and tachycardia
during intubation
 Decreased hemodynamic variability both
intraoperatively and postoperatively in
patients receiving clonidine
 These drugs are given just before induction
of anaesthesia
OPIOIDs:
 Frequently used in immediate preinduction period
to suppress autonomic responses to tracheal
intubation.
 It provides control of preoperative anxiety, minimize
anesthetic requirement and provide postoperative
pain relief.
Fentanyl- it is used in the dose of 1 to 2 μg/kg
Alfentanyl- it penetrates brain very rapidly, so
equlibrium between plasma and brain is attained soon
Remifentanyl- it is the opioid of choice in out patient
surgery because of its shortduration of action. It is given
in dose of 0.25 to 1μg/kg.
Disadvantages of Premedication

 Suppress cardiovascular system

 Respiratory depression
 Not closely monitored
 Hard to monitor effects
 Side effects of individual drugs
Drug selection

 Produce reliable sedation and anxiolysis

 Have minimal effects on the
cardiovascular system
 Causes minimal respiratory depression
 Produce analgesia
 Reversibility
Determinants of Drug Choice and Dose

and Pre existing illness

 ANTIMUSCURANIC DRUGS
Used for :
 Antisialogue action
 Avoid bradycardia due to
 anaesthetic agents
 surgical stimulus(occulocardiac reflex, mesenteric
traction)
 β blocked or digitalised patients
 Intermittent Scholine
 Avoid reflex bronchospasm ( for eg. In COPD)
 Children ( due to vagal predominance)
 Disadvantages :
 Dry mouth ,palpitations, arrhythmias, blurred vision
 Central anticholinergic syndrome
 ATROPINE

 Anticholinergic drugs competitively antagonize

the effects of the neurotransmitter acetylcholine
at cholinergic postganglionic sites designated as
muscarinic receptors
 Anti-cholinergics are esters of aromatic acid
combined with an organic base, that block
muscarinic receptors.
 The ester linkage is essential for effective
binding of the anticholinergics to Ach receptors.
this competitively blocks binding by Ach &
prevents receptor activation.
Pharmacological characteristics:-
Cardiovascular:-
 Blockade of M2 receptors in SA node results in
sinus tachycardia.
 ECG -↓PR interval.
 Large doses of anticholinergics can results in
dilatation of cutaneous blood vessels.(atropine
flush)
 A transient slowing of heart rate in response to
low doses of anticholinergics has been reported.
(d/to weak peripheral agonist effects)
RESPIRATORY SYSTEM:-
 Anticholinergics inhibits the secretions of respiratory tract
mucosa from the nose to bronchi.
 Relaxes bronchial smooth musculature.it reduces airway
resistance leads to ↑in anatomic dead space.
CEREBRAL:-
 Crosses blood brain barrier
 Can cause spectrum of CNS effects from stimulation to
depression.
 Central anticholinergic syndrome: cause restlessness,
hallucinations, seizures, disorientation or signs of
depression such as stupor, coma and respiratory
depression due to Acetylcholine release in CNS
 Stimulation may present as excitation,
restlessness/hallucination.
 Depression can cause sedation & amnesia.
GASTROINTESTINAL:-

 Salivary secretions are markedly decreased,

gastric secretions are also decreased but large
doses are necessary.
 Decrease intestinal motility & peristalsis.
Prolong gastric emptying time.
 Lower esophageal sphincter pressure is
reduced.
OTHER SYSTEMS:-

OPTHALMIC:-
 Causes mydriasis.

GENITO URINARY:-
Decrease ureter & bladder tone lead to urinary
retention.

THERMOREGULATION:-
Inhibition of sweat glands may lead to rise in body
temperature.(atropine fever)
 As a premedication atropine is administerd
IV /IM in a range of 0.01-0.02mg/kg body wt.

 Atropine should be used cautiously in pt with

narrow angle glaucoma prostatic hypertrophy
/bladder neck obstruction.
GLYCOPYRROLATE:-
 It is a synthetic quaternary ammonium
compound containing mandelic acid.
 Usual dose of it is 0.005-0.01mg/kg.
 Due its structure it cant cross blood brain barrier
& devoid of CNS & ophthalmic activity.
 Potent inhibition of salivary gland & respiratory
tract secretions is the prime reason for using it
as premedication.
 HR usually ↑ after an IV administration but not in
IM use.
 Longer duration of action than atropine.
(2-4 hrs Vs. 30 min )
 Comparison between them:-

Atropine Glycopyrrolate.
Tachycardia +++ ++
Bronchodilation ++ ++
Sedation + 0
Antisialagogue ++ +++
effect
Comparative Effects of Anticholinergics
Undesirable Side Effects of Anticholinergics
BENZODIAZEPINES
 Most commonly used premedication drug
 They act as
Anxiolytic
Sedative
Amnesic
Hypnotic

 Classification
Long acting – diazepam, Alprazolam
Medium acting – temazepam
Short acting - midazolam
 Benzodiazepines enhance the effects of
GABA on GABA receptor
 Thus they increase the frequency of
chloride channel opening
 Increased chloride ions cause neuronal
hyper-polarisation and thus inhibition
Stage 3 sleep is increased
Stage 4 sleep and REM sleep decreased
MIDAZOLAM:-
 Most commonly used benzodiazepine in pediatric pt, iv sedation,& induction
of anesthesia.
 Water soluble benzodiazepine with an imidazole ring 2-3 times more
potent than diazepam.
 At blood pH, drug becomes lipid soluble and penetrates brain rapidly in
90 seconds – peak effect 2- 5 mins
 Short acting i.e. half life is 1-3 hrs. For pre operative medication
midazolam 0.5 mg /kg administered orally 30 mins before induction
provides reliable & Anxiolysis in children.
 IM dose is 0.05-0.1 mg/kg. IV dose in adult is 1-2.5 mg before induction
of anesthesia.
 It is a minimal CVS depressant reduces BP, CO & PVR ,but when
combined with opioids markedly reduces BP & PVR .
 It reduces MAC of volatile anesthetics as much as 30%
 Has hepatic elimination
Diazepam
 Insoluble in water so formulated in propylene
glycol, which is very irritant to veins.
 Bioavailability 100%
 Protein binding 90-95%.
 Diazepam has largely been replaced by
Midazolam in premedication because it is
in soluble in water, pain in IM/IV injection
&phlebitis is often occur after IV injection.
Comparison of Pharmacologic Variables of Benzodiazepines

DIAZEPAM LORAZEPAM MIDAZOLAM

Dose equivalent (mg) 10 1–2 3–5

Time to peak effect after 1–1.5 2–4 0.5–1

oral dose (hr)

Elimination half-time (hr 20–40 10–20 1–4

FENTANYL.
 It is a phenyl piperidine derivative synthetic
opioid agonist .
 It is 75- 125 times more potent than morphine.
 It has more rapid onset (2-5 min)& shorter
duration of action(1-2 hrs) due to its rapid
redistribution to inactive tissue sites (fat,
muscles & lungs).
 Extensively metabolized by methylation
producing norfentanyl & excreted by kidneys.
 It can be given by IM or IV route.
 To blunt circulatory responses to :-
1. Direct laryngoscopy for intubation.
2. During sudden changes in the level of surgical
stimulation.
Side effects:-
 Bradycardia:-it may lead to occasional decrease
in BP& CO.
 Can produce significant muscle rigidity.(wooden
chest syndrome)
 Stimulation of CTZ is responsible for high
incidence of nausea & vomiting.
 Pruritis:- prominent around the nose.
TRAMADOL:-
 Centrally acting analgesic.
 Low affinity for mu opioid receptors.
 It inhibits reuptake of NA & 5 HT. Thus activates
mono aminergic spinal inhibition of pain.
 Naloxone antagonizes only 30 % of effect of
tramadol.
 Adult dose is 50 -100 mg 4-6 hrly. not greater
than 400 mg in 24 hrs. For children 1-2 mg /kg
4-6 hrly.
 Approx 1/10th as potent as morphine.
 T ½ is 3-5 hrs.
 Side effects are dizziness, nausea,
vomiting sleepiness, dry mouth &
sweating.
 Indicated in medium intensity short
lasting pain due to diagnostic
procedures, injury ,surgery etc as well
as chronic pain like cancer pain.
ONDANSETRON
 ONDANSETRON is a carbazalone derivative
structurally related to serotonin
 Selectively block serotonin 5-HT3 receptors
(peripheral abdominal vagal afferents and central
CTZ receptors), with little or no effect on dopamine
receptors
 Has specific 5HT3 subtype receptor antagonist
prosperities without altering dopamine ,histamine
adrenergic or cholinergic receptor activity.
 The most commonly side effects are headache,
diarrhea,& transient in liver transaminase enzyme.
 Rarely, cardiac arrhythmias have been reported
after IV administration
 Sedation, hypotension, dysphoria & extra pyramidal symptoms
that may accompany administration of alternative antiemetic drugs
promethazine, droperidol ,metoclopramide do not accompany
administration of ondansetron .
 Should be reserved for symptomatic treatment of nausea or
vomiting as studies indicate no differences in outcome when
antiemetics are administered either for symptomatic treatment or
prophylactically

 But can be used in procedures/ patients at risk for nausea and

vomiting

 Ondansetron 4 to 8 mg IV immediately before the induction of

anesthesia is highly effective in PONV

 In children dose of ONDS is 0.1 mg /kg up to 4 mg for prophylaxis

& T/t of PONV
 It is eliminated in urine & feces mostly as metabolites T1/2 being 3-
5hrs & duration of action 4-12 hrs
H2 Receptor Antagonists
 Ranitidine is a H2 receptor antagonist that produce
selective and reversible inhibition of H2 receptor thus
inhibiting gastric secretion in response to acetylcholine,
histamine, or gastrin and reducing concentration of
hydrogen ions.
 In preoperative period H2 receptor antagonist have
been administered to increase the pH & decrease
gastric fluid volume of gastric fluid before induction &
thus decrease the risk of acid pneumonitis
 Rapid I.V. administration may cause bradycardia
&hypotension most often in critically ill & elderly pts
 Can sometimes causes mental confusion, particularly
in elderly patient and usually within 48 hours of the first
dose
 Duration of action is 24 hrs

 Side effects are headache, diarrhea,

constipation & dizziness. Hepatic injury, CNS
effects & hematological changes are rare,
mostly seen in elderly.
Metoclopramide
 Metoclopramide is a central dopamine antagonist and
peripheral cholinomimetic that
speeds gastric emptying &decreases gastric fluid volume
increases the tone of the lower esophageal sphincter, and
prevents or alleviates nausea and vomiting
 Dose of 10–20 mg of metoclopramide (0.25 mg/kg) is
effective orally, intramuscularly, or intravenously (injected
over 5 min)
 Antimuscarinic drugs block its gastrointestinal side effects
 Rapid I.V. injection may cause abdominal cramping
 Can induce hypertensive crisis in pheochromocytoma
 Other side effects: sedation, nervousness & extrapyramidal
signs
α2 RECEPTOR AGONISTS
 Action : they decrease noradrenaline release in both
central and peripheral symp. N.
 CNS :
 tractus solitarius – hypotension & bradycardia
 Locus coerulus – sedation
 Spinal & supraspinal level(non opioid) - Analgesia
 Vagal nuclei
 Peripheral :
 Decrease cardiac rate
 Decrease smooth muscle tone
 Increase coronary blood flow
 Induce diuresis
 Platelet aggregation
 Decrese MAC requirements
 Attenuate sympathoadrenal responses
associated with intubation and surgery

 Side effects : dry mouth, sedation,

depression, bradycardia, rebound
hypertension
 Clonidine
 Clonidine is an imidazoline derivative with
predominantly α2-adrenergic agonist activity
 Highly lipid soluble and readily penetrates
the blood–brain barrier and the placenta
 Decreases sympathetic activity, enhances
parasympathetic tone, and reduces
circulating catecholamines
 Reduces intraoperative hypertension &
tachycardia, causes sedation and hypnosis
 Premedication for cardiac Pts
 Whatever the drug patient is taking, should be taken on
the day of surgery
 For pts with known or suspected Coronary artery
disease, beta blockers may be added
 b-blockers reduces mortality & incidence of non fatal MI
It is probably a drug class effect or hemodynamic effect.
 C\I are- known allergy to b-blockers, 2nd or 3rd degree
heart block, CHF, acute bronchospasm, low systolic BP
& bradycardia.
 B-blockers may be started several days prior to surgery.
 IV metoprolol may be given just prior to surgery if
inadequate blockade achieved with oral medication.
Premedication for Diabetes Pts
 Peri op stress may ↑blood. glucose.

 A plan for perioperative insulin & glucose

management must be done.

 There are several methods of doing this

 To administer 1/4th to ½ of the usual daily dose of
insulin in the morning of surgery & begin an
infusion of glucose containing fluid.
 A second way is to administer no insulin or no
glucose preop and to measure blood glucose
frequently during anesthesia and correct
accordingly
 third method is to begin an infusion of insulin and
glucose immediately preoperatively & check
blood glucose frequently.
PREMEDICATION FOR DAY
CARE SURGERY
Anxiolysis and sedation
 Most widely used drugs are benzodiazepines and
barbiturates
 Benzodiazepine like midazolam is commonly used
because of its short half life and rapid recovery.
Diazepam, triazolam, temazepam are also used but less
effective than midazolam.
 α2- adrenergic agonists are also used, it reduces the
anesthetic requirement and produce significant sedation,
and attenuates sympathoadrenal stimulation during
intubation and surgery.
 Oral clonidine which is selective α 2 agonist is the
commonly used drug.
 Dexamedetomidine (selective α 2 agonist) is also used
which has shorter duration of action than clonidine. It
also has analgesic effect.
Analgesic
OPIOIDs:
 Frequently used in immediate preinduction
period to
Remifentanyl- it is the opioid of choice in out
patient surgery because of its short duration of
action. It is given in dose of 0.25 to 1μg/kg.
Fentanyl- it is used in the dose of 1 to 2 μg/kg
Alfentanyl- it penetrates brain very rapidly, so
equlibrium between plasma and brain is attained
soon
NON OPIOIDS:
 NSIADS are the non opioids frequently used
Selective COX2 inhibitors like roficoxib,
celicoxib are preferred .
 Ketarolac is used in many surgery, which is
more effective in ear surgery
 Rectal preparations are used in children.
Nausea and vomiting

 Ondensetron 4mg is used commonly

 Metaclopromide(10 mg) and domperidone are
prokinetic drugs which facilitates gastric and
small bowel motility. It also has
antidopaminergic action.
 Anti cholinergics like atropine, glycopyrrolate,
scopolamine are also used because of its
vagolytic and antisialagogic activity.
 Antihistaminic drug which act on vomiting center
and vestibular pathways. Hydroxyzine is the
commonly used antihistamine
Prevention of aspiration

H2 receptor antagonists like ranitidine is used to

reduce gastric secretion.
Metoclopramide because of its antidopaminergic
action, reduces gastric content by stimulating
gastric emptying without altering pH
Antacids are used to increase the pH
Premedication for Neuro S Pts
Preop medication that produces sedation or ventilatory depression
should be avoided in pt with IC tumor(pts with raised ICP)

Opioid induced hypoventilation can lead to accumulation of Co2

leads to ↑ICP.

Prophylactic phenytoin may be required (loading dose 15mg/kg

followed by a single dose 3-4 mg/kg)

Corticosteroids: Dexamethasone (effective for localized cerebral

edema surrounding tumors; requires 12–36 hours).

Esmolol infusion or bolus may be used to reduce the heart rate and
blood pressure response to laryngoscopy and intubation
Premedication for pediatric pts
 Premedication has been given to the pediatric
pt for following objectives:-
1. To block possibly harmful vagal reflexes.
2. To dry secretions in respiratory tract.
3. To produce sedation, easy separation,&
facilitate induction of anesthesia.
4. To supplement analgesia & reduce the
requirement for general anesthetic drugs.
The 1st two objectives are achieved by the use of
anticholinergic drugs. others may be effected
by the narcotic, hypnotic or tranquilising
 Atropine:-most useful drugs for pediatric patients.it
can be given by oral, rectal, subcutaneous, IV, IM &
intratracheal routes.In a dose of 0.02 mg/kg. It is
effective in preventing bradycardia that follows
administration of succinylcholine, instrumentation of
airways or traction of the eye muscles.
 Glycopyrrolate:-also used for premedications for
children.it has been reported less tachycardia than
atropine.cause greater drying effects in
secretions.more effective in reducing the volume &
acidity of gastric content.dose-0.005-0.01mg/kg
SEDATIVE DRUGS:-
 The medications selected according to
following general guidelines:-
1. Infants less than 6 months of age do not
require sedative premedications.
2. Children do not like intramuscular
injections & nasal drops.
3. Older children(greater than 3 yrs) do not
like rectal applications of drugs.
4. Should not be given to those with problem
of airway or ventilation or those with CNS
disease
 Midazolam:-most commonly used
sedative agent.it produces
sedation,anxiolysis,& anterograde
amnesia.facilitate separation of children
from parents. it reduces post operative
emotional and behavioral disturbances.it
smoothens induction of anesthesia&
reduce the dose of anesthetic drugs.
Dose 5mg/kg PO.0.1mg/kg IV
 Opioids – Narcotic analgesics produce significant
respiratory distress specially in younger infants and
increase the incidents of post operative vomiting in
all patients. A major additional disadvantage of
these drugs is that they have commonly been
given by intramuscular injection , a painful
procedure not likely to produce tranquility and
cooperation in child.
 The fentanyl oral in a dose of 15-20 μgm/kg has
been studied as a pre operative medication and
found to produce sedation and reduce anxiety.
Respiratory rate was decreased but the
hemoglobin/ oxygen saturation level was not
significantly reduced. Nausea , vomiting , and
purities limit the usefulness of the fentanyl.
 Opioids are not routinely used in children.
Premed. for psychiatric pts
 Opioids should avoided in pts being treated
with MAOIs.
 In the absence of specific indication of Ach
drugs in premedication, is probably not
necessary.
 BZDs are acceptable for anxiety.
 In ECT:
Avoid sedative premedication.
glycopyrrolate may be used to reduce secretions
& to counteract bradycardia.
Drugs and Doses Used for Pharmacologic Premedication: summary
Thank you