Medication Administeration Part II

Anti - inflammatory drugs #1
◊ Inflammation is a reaction to tissue injury caused by the release of

chemical mediators (histamines, kinins and prostaglandins).
◊ Causes:
◊ Vasodilation (dilate arterioles) => Redness or erythema.
◊ Increased capillary permeability => swelling or edema.
◊ Pain The five responses to tissue injury are called
◊ Fever the cardinal signs of inflammation: redness,
◊ Loss of function swelling, pain, heat and loss of function.
◊ Medications that inhibit these chemical mediators and decrease the
inflammatory process is called anti-inflammatory drugs.
◊ Anti-inflammatory drugs can be:
◊ Nonsteroidal anti-inflammatory drugs (NSAIDs).
◊ Steroids.
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Nonsteroidal Anti-Inflammatory Drugs (NSAIDs)
◊ Mechanism of action: inhibit the enzyme cyclooxygenase (COX).
◊ COX is the enzyme responsible for prostaglandin synthesis.
◊ Based on its ability to inhibit the specific types of COX enzymes, there
are two main types of NSAIDs:
◊ Nonselective NSAIDs: inhibit both COX-1 and COX-2 enzymes.
E.g., diclofenac, indomethacin, aspirin, ibuprofen, naproxen, …
◊ Selective NSAIDs: inhibit COX-2 enzyme.
E.g., Celecoxib, etoricoxib, …
◊ Absorbed completely, tightly bound to serum protein, have small
volume of distribution, metabolized by CYP2C8/9/19 or glucuronidation.
 COX-2 is an enzyme found at sites of inflammation.
 COX-1 is normally found in stomach, blood platelets, blood vessels, …
◊ Clinical use: has analgesics, antipyretics and anti-inflammatory effect.
◊ Rheumatoid arthritis, osteoarthritis, ankylosing spondylitis,
headache, gout, dysmenorrhea (menstrual pain), pyrexia, … etc.
◊ Contraindications to nonselective NSAIDS: known and/or highly at risk
for coronary artery disease (e.g., heart attack, angina, stroke, …etc.),
renal and hepatic disorder, hypersensitivity, …etc..
◊ Regimen: use lower dose & should not use two NSAIDs at the same time.
◊ Side effect of NSAIDs: mainly due to their mechanism of action.
◊ Cardiovascular: myocardial infarction, stroke, rise blood pressure, …
◊ Gastrointestinal system: dyspepsia, peptic ulcer disease and bleeding.
◊ Renal effect: acute renal failure due to renal vasoconstriction, fluid
and electrolyte abnormality (hyperkalemia and hyponatremia), …
◊ Hepatic (elevate serum aminotransferase) and lung (bronchospasm).
◊ Hematologic: increase bleeding risk, neutropenia, aplastic anemia, …
Steroids:
◊ Includes: prednisolone, hydrocortisone, dexamethasone, …etc.
◊ Mechanism of Action: decreases inflammation by suppression of
neutrophil migration, decreased production of inflammatory mediators
and reversal of increased capillary permeability, suppresses normal
immune response.
◊ Clinical use: asthma (acute exacerbation), rheumatoid arthritis,
osteoarthritis, gout, anaphylaxis, …etc.
◊ Adverse effect: headache, nausea, vomiting, increased appetite, weight
gain, insomnia, increased blood glucose, …etc.
◊ Contraindication: hypersensitivity, serious infections (except meningitis)
◊ Precautions: prolonged treatment will result in adrenal suppression, do
not discontinue abruptly, long-term use in children will result in
decrease growth, use lowest dose possible for shortest time possible, …
Miscellaneous analgesic and antipyretics #1
A. Opioids: tramadol, pethidine, morphine, fentanyl, codeine, …etc.
◊ Mechanism of action: binds to opioid receptors in the CNS, causing
inhibition of ascending pain pathways, altering the perception of and
response to pain.
◊ Clinical use: moderate to severe pain, acute (e.g., postoperative pain)
chronic pain (e.g., cancer pain), …etc.
◊ Adverse reaction: constipation, neurotoxicity (allodynia, delirium,
hallucinations, hyperalgesia, hypersomnolence, tremor, …), pruritis,
respiratory depression, bradycardia, …etc.
◊ Contraindication: hypersensitivity, significant respiratory depression, GI
obstruction including paralytic ileus, bronchial asthma, …etc.
◊ Precaution: prolonged use may lead to physical and psychological
dependence and tolerance, titrate dose to avoid withdrawal, naloxone
is the antidote, regularly administered dose is more effective than prn, ..
Miscellaneous analgesic and antipyretics #2
Miscellaneous analgesic and antipyretics:
B. Nonopioid e.g., paracetamol (acetaminophen).
◊ Mechanism of action: inhibition of the hypothalamic heat-regulating
center, prostaglandin inhibition in the CNS and blocks generation of
pain impulses in the peripheral tissue as well as activation of descending
serotonergic inhibitory pathways in the CNS.
◊ Clinical use: analgesic and antipyretics.
◊ Adverse effect: hepatotoxicity, hypersensitivity, dermatologic, …etc.
◊ Contraindication: hypersensitivity, active liver disease, …etc.
◊ Consideration: adults should not take acetaminophen longer than 10
days and children not longer than 5 days, not to exceed 5 doses/24 hour,
concurrent use of some drugs (e.g., isoniazid, rifampin, phenytoin, …)
may increase the risk of acetaminophen-induced liver damage.

Drugs affecting the gastrointestinal system
◊ Drugs to control gastric acidity and ulcer:
a. Antacids
b. Histamine-2 (H2) receptor antagonists
c. Proton-pump inhibitors (PPIs)
◊ Drugs for nausea and vomiting
◊ Drugs for constipation
◊ Drugs for diarrhea
◊ Drugs for inflammatory diseases
◊ Drugs for hemorrhoid

Drugs to control gastric acidity #1
◊ Gastric acidity and ulcer can be controlled by:
1. Neutralizing secreted acid & decreasing pepsin production
◊ Antacids
2. Decreasing gastric acid secretion
◊ Histamine 2 receptor antagonists (H2RAs)
◊ Proton pump inhibitors (PPIs)
3. Eliminating infectious agents that cause ulcer
◊ Antimicrobials and bismuth eliminate H. pylori infection
4. Protecting mucosal layers: sucralfate
5. Restoring prostaglandin E2 activity: misoprostol

Antacids: alkaline substances that neutralize acids.
◊ Aluminum Hydroxide + Magnesium Hydroxide + Simethicone
◊ Aluminum Hydroxide + Magnesium Trisilicate
◊ Mechanism of action: neutralize gastric acid and decrease pepsin
production.
◊ Clinical use: heartburn associated with mild intermittent
gastroesophageal reflux disease (not for peptic ulcer disease).
◊ Adverse effect: depend upon dose and the duration of therapy.
◊ Magnesium containing antacid: diarrhea and hypermagnesemia.
◊ Aluminum Hydroxide: aluminum retention (renal failure and
anemia), hypophosphatemia, constipation, osteomalacia, …etc.
◊ Contraindication: signs of appendicitis or inflamed bowel or renal
failure, previous hypersensitivity, …etc.
Histamine 2 (H2) receptor antagonists:
◊ Includes: cimetidine, famotidine, ranitidine, …etc.
◊ Mechanism of action: inhibit acid secretion by blocking H2 receptors
on the parietal cell.
◊ Clinical use: heart burn, peptic ulcer disease (PUD), gastroesophageal
reflux disease (GERD), Zollinger-Ellison syndrome, …etc.
◊ Adverse effect: gynecomastia, impotence, B12 deficiency, hepatitis, ...
◊ Contraindication: hypersensitivity, …etc.
◊ Consideration: immunocompromised patients, may have increased
risk of hyper infection of strongyloidiasis, do not administer
simultaneously with antacids (antacids decrease absorption), … etc.

Proton-Pump Inhibitors:
◊ Include: omeprazole, pantoprazole, esomeprazole, lansoprazole, …
◊ Mechanism of action: block acid secretion by irreversibly binding to
and inhibiting the hydrogen-potassium ATPase (H+/K+-ATPase) pump
that resides on the luminal surface of the parietal cell membrane.
◊ Clinical use: gastric and duodenal ulcers, gastroesophageal reflex
disease (GERD) and pathologic hypersecretory conditions.
◊ Used for H. pylori elimination with antimicrobials.
◊ Prevention of NSAIDs associated gastroduodenal mucosal injury.
◊ Adverse effect: increase the risk of clostridium difficle and other
enteric infection, malabsorption of minerals and vitamins
(magnesium, B12, iron, calcium), nephritis, …etc.
◊ Contraindication: hypersensitivity, significant drug interaction, …etc.
Medications used to treat helicobacter pylori:
◊ Combination therapy with antibiotics.
◊ At least two antibiotics and proton pump inhibitor (triple therapy).
◊ Antibiotics: amoxicillin, clarithromycin, metronidazole & tetracycline.
◊ Twice daily for 14 days.
◊ Occasionally:
◊ Bismuth subsalicylate is recommended for patients with peptic
ulcer disease who are known to be infected with H. pylori.
◊ Bismuth does not inhibit and neutralize gastric acid.
◊ Sucralfate; suppress H. pylori and inhibit acid secretion.
◊ Also buffering acid.
◊ Misoprostol: inhibit acid secretion.

Actions of antiulcer medications

Drugs to control nausea and vomiting #1
Drugs to control nausea and vomiting
◊ Called antiemetic agents.
1. 5-HT3 receptor antagonists
2. Dopamine-receptor antagonists
3. Muscarinic antagonist
4. H1 antagonist
5. Corticosteroids
6. Neurokinin-1 receptor antagonists
7. Cannabinoids

Serotonin (5-HT3) receptor antagonists:
◊ Includes: Ondansetron, dolasetron, palonosetron, … etc.
◊ Mechanism of action: blocks serotonin, both peripherally on vagal

nerve terminals and centrally in the chemoreceptor trigger zone.
◊ Clinical use:
◊ After general anesthesia
◊ In patients receiving cancer chemotherapy
◊ Adverse effect: constipation, intestinal obstruction, headache, … etc
◊ Contraindication: hypersensitivity, QT prolongation, … etc.

H1 antagonists:
◊ Includes: diphenhydramine, promethazine, …etc.
◊ Mechanism of action: block the action of histamine at the H1
receptor.
◊ Indication: motion sickness, postoperative, radiation sickness, …
◊ Contraindication: hypersensitivity, neonates or premature infants,
breast-feeding, … etc.
◊ Side effect: anticholinergic (antimuscarinic) effects.
◊ Blurred vision, xerostomia (dry mouth), urinary retention
◊ Impotence, tachycardia
◊ Gastrointestinal effects (e.g., nausea, constipation)
◊ CNS effects (e.g., sedation, agitation, confusion, delirium), …

Anticholinergic agent or muscarinic receptor antagonists:
◊ Scopolamine (hyoscine) = hydrobromide and butylbromide.
◊ Blocks the activity of the muscarinic acetylcholine receptor.
◊ Also, dries secretions, antagonizes histamine and serotonin.
◊ Indication: motion sickness and postoperative.
◊ Sometimes used before surgery to decrease saliva.
◊ Side effect: blurred vision, dilated pupils, dry mouth, sedation, …
◊ Contraindication: hypersensitivity, narrow angle glaucoma, bowel or

pyloric obstruction, paralytic ileus, prostatic hypertrophy, ….
Dopamine receptor antagonists:
◊ Includes: metoclopramide, chlorpromazine, prochlorperazine
◊ Metoclopramide also called prokinetic drugs.
◊ Action: blocks dopamine receptors in chemoreceptor trigger zone of the
CNS, enhances response to acetylcholine of tissue in upper GI tract
causing enhanced motility and accelerated gastric emptying without
stimulating gastric, biliary or pancreatic secretions and increases lower
esophageal sphincter tone.
◊ Indication: emetogenic chemotherapy, postoperative, gastroesophageal
reflux, hiccups (?), radiation therapy, … etc.
◊ Adverse effect: CNS depression (drowsiness, fatigue, lassitude, dizziness
and confusion), extrapyramidal reaction (dystonic reactions, Akathisia
(motor restlessness), Tardive dyskinesia, …
◊ Contraindication: hypersensitive, GI obstruction, seizure, …
Drugs to prevent and treat constipation #1
◊ Drugs to prevent and treat constipation is called laxatives.
◊ And also:
◊ For colon evacuation before rectal/bowel examination.
◊ For prevention of straining, e.g., after anorectal surgery
◊ To reduce painful elimination, e.g., hemorrhoids, anorectal lesion
◊ For removal of ingested poisons, … etc.
◊ Laxatives can be:
◊ Stimulants, e.g., bisacodyl
◊ Saline laxatives, e.g., magnesium salts and phosphates
◊ Stool softeners, e.g., docusate
◊ Bulk-forming, e.g., polycarbophil, psyllium, methylcellulose
◊ Osmotic cathartics, e.g., lactulose, polyethylene glycol

Bulk-forming: polycarbophil, psyllium, methylcellulose
◊ Act primarily in small and large intestine.
◊ Absorbing water and increasing fecal mass.
◊ May increase colonic bacteria growth (increase fecal mass).
◊ Their effect is similar to that of increased intake of dietary fiber.
◊ Adverse effect: anaphylaxis, abdominal cramps, diarrhea, intestinal
obstruction, electrolyte imbalance, …etc.
◊ Contraindications: Hypersensitivity, fecal impaction, GI obstruction
Stool softeners or surfactant agents, e.g., docusate:
◊ Acts in small or large intestine.
◊ Decrease the surface tension of the fecal mass, facilitating
penetration of fat and water into stool.
◊ Adverse effect: rare, but rash around the anus or rectal irritation.

Saline laxatives, e.g., magnesium salts and phosphates:
◊ Acts in small and large intestine, poorly and slowly absorbed
◊ Causes cholecystokinin hormone release from duodenum
(stimulates fluid secretion, motility)
◊ Also, increase osmotic pressure in intestinal lumen, resulting in
retention of water, distends bowel and stimulates peristalsis.
◊ Adverse effect: rare, but accumulation of magnesium may lead to
renal magnesium intoxication
Osmotic cathartics, e.g., lactulose, polyethylene glycol:
◊ Act in colon and similar action as saline laxatives.
◊ Exerts an osmotic effect, pulling water into the colon and
stimulating peristalsis.
◊ Adverse effect: Abdominal cramps and pain, abdominal distention,
bloating, diarrhea, eructation, flatulence, nausea, vomiting, …
Stimulants, e.g., bisacodyl, castor oil and glycerin:
◊ Irritate the GI mucosa, pull water/electrolyte into the colon and
enhance intestinal motility and stimulate peristalsis.
◊ May act directly on intestinal mucosa.
◊ Adverse effect: abdominal pain, diarrhea, flatulence, ischemic
colitis, headache, …etc.
Clinical alert:
• For a patient on laxatives:
• Assess patient for abdominal distention, presence of bowel
sounds, and usual pattern of bowel function.
• Assess color, consistency, and amount of stool produced.

Drugs to control diarrhea #1
◊ Drugs to control diarrhea is called antidiarrheal drugs.
◊ Opioid agonist: the most effective agents e.g., loperamide.
◊ For acute and chronic diarrhea.
◊ Mechanism of action: acts the intestinal muscles via opioid receptor:
◊ Inhibit peristalsis and prolong transit time.
◊ Reduces fecal volume, increases viscosity & diminishes fluid loss.
◊ Demonstrates antisecretory activity.
◊ Increases tone on the anal sphincter.
◊ Adverse effect: abdominal cramp, constipation, nausea, dizziness, …
◊ Contraindication: hypersensitive, abdominal pain without diarrhea,
children <2 years, acute dysentery, acute ulcerative colitis, bacterial
enterocolitis (caused by Salmonella, Shigella and Campylobacter);
pseudomembranous colitis due to broad-spectrum antibiotic use, …
Drugs to control diarrhea #2
Adjuvant drugs for diarrhea:
◊ Bismuth salt/subsalicylate: have antibacterial and antiviral activity.
◊ Antisecretory action (stimulate fluid and electrolyte absorption).
◊ Anti-inflammatory effect because of salicylate component (via
inhibition of prostaglandin synthesis).
◊ Antibacterial drugs:
◊ when diarrhea lasts longer than 48 hours.
◊ If six or more loose stools in 24 hours.
◊ Diarrhea is associated with fever, bloody and/or pus.
◊ Miscellaneous:
◊ Oral Rehydration Solution (ORS).
◊ Zinc Sulphate.

Antiviral agents #1
◊ Antiviral is a class of medication used to treat viral infections.
◊ Its exert their actions at several stages of viral replication.
E.g., block viral attachment, penetration, nucleic acid synthesis,
integration, virion release, …etc.
A. Drugs for herpesviruses: acyclovir, famciclovir, ganciclovir, …etc.
◊ Mechanism of actions: inhibits DNA synthesis and viral replication.
◊ Clinical use: herpes simplex virus, varicella-zoster virus, Epstein-Barr
virus, cytomegalovirus, …etc.
◊ Adverse effect: acute kidney injury (interstitial nephritis or renal
tubular necrosis), neurotoxicity (agitation, confusion, dysarthria,
hallucination, aphasia, ataxia, myoclonus, tremor), thrombotic
thrombocytopenic purpura, nausea, pruritis, flatulence, diarrhea, …
◊ Contraindications: hypersensitivity, …etc.
Antiviral agents #2
B. Drugs for HIV
◊ Anti-retroviral therapy is the treatment of HIV infected individuals
with anti-retroviral drugs, also called HAART (highly active
antiretroviral treatment).
1. Reverse transcriptase inhibitors
◊ Inhibit the activity of reverse transcriptase, which is an enzyme
used to generate DNA from RNA via reverse transcription.
a. Nucleoside reverse transcriptase inhibitors (NRTIs):
◊ Zidovudine, abacavir, lamivudine, stavudine, emtricitabine, ..
 Lamivudine is active in hepatitis B.
b. Nucleotide reverse transcriptase inhibitors: tenofovir.
c. Nonnucleosides reverse transcriptase inhibitors (NNRTIs)::
◊ Efavirenz, nevirapine, … etc.

Antiviral agents #3
Side effects:
◊ Zidovudine, AZT: anemia, headache, asthenia, myalgia, myopathy, …
◊ Lamivudine, 3TC: least toxic, but GI effects, neutropenia, …
◊ Efavirenz: CNS dysfunction, skin rash, elevate plasma cholesterol, …
2. Protease inhibitors: prevent maturation of new viruses by
interfering with enzymes that cleave proteins (protease).
◊ Drugs and their side effects:
◊ Atazanavir: GI distress, peripheral neuropathy, skin rash,
hyperbilirubinemia.
◊ Ritonavir: induces CYP 1A2 and inhibits the major P450 isoforms
(3A4 and 2D6)
◊ Darunavir: GI upset, headaches, skin rash, constipation
◊ Lopinavir/ritonavir: diarrhea, nausea
Antiviral agents #4
3. Integrase strand transfer inhibitors: raltegravir, dolutegravir, …
◊ Prevent the integration of viral genome into host cell DNA by
inhibiting the enzyme integrase.
◊ Adverse effect: nausea, headache, diarrhea, pyrexia, …
4. Entry and fusion inhibitor: block the entry of HIV into cells.
◊ Enfuvirtide: binds to gp41 and inhibits the fusion HIV to CD4+ cells.
◊ Maraviroc: blocks the binding of the gp120 HIV protein to CCR5
on macrophage surface to prevent viral entry.
◊ Adverse effects:
◊ Enfuvirtide: hypersensitivity, increased incidence of bacterial
pneumonia, …
◊ Maraviroc: cough, muscle and joint pain, increases in hepatic
transaminases, ...

Antimalarial agents #1
◊ A drug used for the prevention and treatment of malaria infection.
◊ Most drugs target the erythrocytic stage of malaria infection:
◊ Which is the phase of infection that causes symptomatic illness.
A. Quinoline derivative: chloroquine, quinine, mefloquine, primaquine, ..
◊ Mechanism of action: accumulating in the parasite food vacuole and
forming a complex with heme that prevents crystallization in the
plasmodium food vacuole.
◊ Inhibit heme polymerase activity => cytotoxic-free heme accumulate.
◊ Have activity against the erythrocytic stage of infection.
◊ Primaquine also kills intrahepatic forms and gametocytes.
◊ Eliminate dormant hypnozoites (prevent relapse).
◊ Quinine is the drug of choice for severe malaria, next to artesunate.

◊ Adverse effect of quinoline derivate antimalaria:
◊ Chloroquine: headaches, dizziness, GI upset, pruritis, …
◊ Quinine: tinnitus, dizziness, disturbed vision, hypoglycemia, ...
◊ Primaquine: hemolytic anemia, GI upset, arrhythmia, ...
◊ Contraindicated for pregnancy, breastfeeding & < 6 months child.
B. Artemisinin derivatives: artemether, artesunate, … etc
◊ Mechanism of action: bind to iron, break down peroxide bridges,
lead to the generation of free radicals that damage parasite proteins.
◊ Kill blood stages of all species, also active against gametocytes.
◊ Clinical use: severe malaria (IV artesunate is a first-line therapy).
◊ Adverse effect: hemoglobinuria, jaundice, acute renal failure, …etc.
◊ Contraindication: hypersensitivity.
C. Antimicrobials:
◊ Includes: doxycycline, tetracycline and clindamycin.
◊ Mechanism of action: inhibits protein synthesis.
◊ Typically paired with fast-acting antimalarials (usually quinine).
◊ Doxycycline has a longer half-life than tetracycline, so is used more
commonly.
D. Antifolates:
◊ Includes: sulfonamides, pyrimethamine, proguanil and dapsone.
◊ Mechanism of action: inhibit dihydrofolate reductase and
dihydropteroate synthase, resulting in inhibition of folic acid
synthesis.
• Coartem is a coformulation of artemether and lumefantrine with

activity against plasmodium falciparum.

Anthelminthics #1
◊ A group of antiparasitic drugs used to prevent and treat worms.
◊ Common anthelmintics and its mechanism of action:
A. Mebendazole: ↓ glucose uptake and ↓ microtubular structure.
B. Albendazole: ↓ glucose uptake and ↓ microtubular structure.
C. Pyrantel: neuromuscular agonist → spastic paralysis.
D. Ivermectin: bind glutamate-gated Cl ion channel, cause paralysis.
E. Praziquantel: ↑ Ca2+ influx, ↑ vacuolization.
◊ Clinical use:
◊ Cestodes, e.g., tapeworms => taeniasis.
◊ Trematodes, e.g., flukes => schistosomiasis.
◊ Nematodes: hookworm, ascariasis (roundworm), trichuriasis
(whipworm), enterobiasis (pinworm), onchocerciasis or river
blindness, strongyloidiasis, …etc.
Anthelminthics #2
Adverse effect of common anthelmintics:
◊ Mebendazole: rarely gastrointestinal upset (pain and diarrhea).
◊ Albendazole: headache, increased liver enzymes, GI upset, …
◊ Pyrantel: rarely GI upset, dizziness, headache, …
◊ Ivermectin: pruritus, lymphadenitis, asthenia, dizziness, GI upset, …
◊ Praziquantel: headache, dizziness, drowsiness, GI upset, …
Contraindication:
◊ Praziquantel: hypersensitivity, with strong CYP450 inducers (rifampin).
◊ Other drugs: hypersensitivity
Reading assignment: diethylcarbamazine, levamisole, …

Miscellaneous antiprotozoal agents
◊ Tinidazole: for amebiasis, giardiasis and vaginal trichomoniasis.
◊ Cause cytotoxicity by damaging DNA, prevent further DNA synthesis.
◊ Adverse effect: metallic taste, vulvovaginal candidiasis, flatulence, …
◊ Diloxanide: amebicide with unknown mechanism of action.
◊ Used mainly for asymptomatic amebiasis.
◊ Miltefosine: for Leishmaniasis, exact mechanism unknown.
◊ Likely interaction with phospholipids in parasitic cell membranes
and inhibition of mitochondrial function.
◊ Sodium stibugluconate: leishmaniasis, exact mechanism is unknown.
◊ Proposed mechanisms: affects glucose metabolism, fatty acid beta
oxidation and ATP formation: activation of host immune system.
• Reading assignment: iodoquinol and pentamidine.

Autonomic nervous system drugs
1. Stimulation of the sympathetic nervous system:
◊ Called adrenergic agents or sympathomimetics.
◊ Produce the classic symptoms of the fight-or-flight response.
2. Inhibition of the sympathetic nervous system:
◊ Called adrenergic-blocking agents or adrenergic antagonists.
◊ Sympatholytic is another name for adrenergic antagonists.
◊ Produce actions opposite those of the sympathomimetics.
3. Stimulation of the parasympathetic nervous system:
◊ Called cholinergic or parasympathomimetic.
◊ Produce the classic symptoms of the rest-and-digest response.
4. Inhibition of the parasympathetic nervous system:
◊ Called cholinergic-blocking agents or anticholinergics.
◊ Parasympatholytic is another name for anticholinergics.
Adrenergic agents #1
Selected adrenergic drugs:
Drug Primary receptor subtype Primary use

Epinephrine Alpha and beta Cardiac arrest, anaphylaxis
Albuterol Beta2 Asthma
Dopamine Alpha1 and beta Shock
Norepinephrine Alpha and beta1 Shock
Dobutamine Beta1 Cardiac stimulant
Methyldopa Alpha2 in CNS Hypertension
Phenylephrine Alpha Nasal congestion
Pseudoephedrine Alpha and beta Nasal congestion
Adrenergic agents #2
Adrenaline or epinephrine:
◊ Mechanism of action: stimulates alpha1, alpha2, beta1 and beta2-
adrenergic receptors resulting in relaxation of smooth muscle of the
bronchial tree, cardiac stimulation (increasing myocardial oxygen
consumption), …etc.
◊ Clinical use: anaphylaxis, hypotension or shock, cardiac arrest, asthma
(acute severe), bradycardia, …etc.
◊ Adverse reaction: increased cardiac work, palpitations, tachycardia,
vasoconstriction, diaphoresis, pallor, piloerection, tissue necrosis at
injection site, drowsiness, tingling sensation, …etc.
◊ Contraindication: no absolute contraindication, but precautions.
• Do not inject into the buttock: may not effectively treat anaphylaxis
and has been associated with Clostridial infections (gas gangrene).
• Preferred injection site is anterolateral aspect of the thigh.
Anticholinergic drugs
◊ Drug that inhibit the actions of acetylcholine in the brain.
◊ Cholinergic-blocking drugs (anticholinergics) and its primary use:
◊ Atropine: poisoning with anticholinesterase agents, bradycardia
(to increase heart rate), inhibit salivation and secretions, …etc.
◊ The primary goal in cholinergic poisonings is reversal of
bronchorrhea and bronchoconstriction.
◊ Atropine has only effect on the muscarinic receptors.
◊ Atropine has no effect on the nicotinic receptors.
◊ Concurrent of pralidoxime is recommended.
◊ Adverse effect: tachycardia, dry mouth, constipation, …etc.
◊ Contraindication: hypersensitive, glaucoma, BPH, GI obstruction, ...
◊ Ipratropium: asthma.
◊ Scopolamine (hyoscine): motion sickness.

Medicines used in anesthesia #1
◊ Anesthesia is a medical procedure performed to put the patient in a
state of controlled, temporary loss of sensation or awareness that is
induced for medical purposes, e.g., For surgical procedures.
◊ Anesthetics: drugs that produce loss of sensation and motor activity.
◊ The are two broad categories of anesthesia: local and general.
1. General anesthesia (GA): drugs that cause loss of sensation to the
entire body, usually resulting in loss of consciousness.
◊ Appropriate for most major surgical procedures.
◊ Goal: hypnosis, amnesia, analgesia, muscle relaxation, …etc.
◊ GA has 3 phases: induction, maintenance and emergence.
◊ Drugs: nitrous oxide (inhalation), benzodiazepines (diazepam),
opioids (fentanyl) and miscellaneous (ketamine, propofol).
2. Local anesthesia: local anesthesia occurs when sensation is lost to a
limited part of the body without loss of consciousness.
Medicines used in anesthesia #2
◊ Local anesthetics act by blocking sodium channels.
◊ Classification of local anesthetics:
A. Amides: e.g., lidocaine, bupivacaine, prilocaine, …etc.
◊ Adverse effect: burning and stinging at injection site, headache,
shivering, nausea, vomiting, bronchospasm, dyspnea, …etc.
◊ Contraindication: hypersensitivity, local infection at the site of
injection, shock, sepsis, …etc.
B. Esters: benzocaine, procaine, tetracaine, …etc.
◊ Adverse effect: burning and stinging at injection site, allergic
contact dermatitis, …etc.
◊ Contraindication: hypersensitivity, do not use over (deep or
puncture wounds, animal bites, infections, serious burns or
lacerations), do not use for teething, children < 2 years of age …
C. Miscellaneous: ethyl chloride, pramoxine, …etc.
Mechanism of action
of local anesthetics.

Drugs act on respiratory system #1
◊ Bronchodilators (smooth muscle relaxants):
◊ Beta-adrenergic agonists
◊ Anticholinergics
◊ Methylxanthine
◊ Anti-inflammatory drugs:
◊ Leukotriene antagonists
◊ Corticosteroids
◊ Mast cell stabilizers
◊ Antitussive, expectorant and mucolytics.

Adrenergic: albuterol (salbutamol), terbutaline, salmeterol, …
◊ Mechanism of action: relaxes smooth muscle of bronchi and

bronchioles by action on beta2-receptors.
◊ Clinical use: asthma (acute exacerbation), bronchospasm due to

anaphylaxis, chronic obstructive pulmonary disease, …
◊ Adverse effects: tremor, cardiac stimulation (angina, tachycardia and

palpitations), CNS stimulation (agitation, anxiety, insomnia), …
◊ Contraindications: hypersensitivity, cardiac tachydysrhythmias, ...
◊ Caution: hypertension, hyperthyroidism, diabetes mellitus, ...

◊ Anticholinergics (e.g., ipratropium bromide): blocks the muscarinic
acetylcholine receptors in the smooth muscles of the bronchi in the
lungs, inhibiting bronchoconstriction and mucus secretion.
◊ Xanthine (theophylline or aminophylline): bronchodilation (by
inhibiting phosphodiesterase) and suppression of the response of the
airways to stimuli .
◊ And also, theophylline increases the force of contraction of
diaphragmatic muscles through enhancement of calcium uptake
through adenosine-mediated channels.
◊ Corticosteroids (e.g., beclomethasone, dexamethasone, hydrocortisone,
prednisone, …) suppress the release of inflammatory mediators, block
the generation of cytokines and decrease the recruitment of airway
eosinophils.
◊ Also increase the sensitivity of beta2-adrenergic receptors, which
increases the effectiveness of beta2-adrenergic bronchodilators.
Antitussives or cough suppressants:
◊ Antitussive is a medication that suppress or control cough.
◊ Can be opioid (e.g., codeine) or nonopioid (e.g., dextromethorphan).
◊ Mechanism of action: decreases the sensitivity of cough receptors
and interrupts cough impulse transmission by depressing the
medullary cough center through sigma receptor stimulation.
◊ Clinical use: dry, hacking, nonproductive cough.
◊ Adverse effect of dextromethorphan: dizziness, drowsiness,
nervousness, restlessness, gastrointestinal upset, …etc.
◊ Contraindications to dextromethorphan: hypersensitivity, significant
drug interactions (linezolid).
• Reading assignment: expectorants and mucolytic.

Medications for allergic rhinitis:
◊ Histamine H1 antagonist: diphenhydramine and chlorpheniramine.
◊ Mechanism of action: competes with histamine for H1-receptor sites
on effector cells in the respiratory tract.
◊ Adverse effect:
◊ Anticholinergic (antimuscarinic) effects: blurred vision,
xerostomia, urinary retention, tachycardia, constipation, agitation
or drowsiness, delirium, thickening of bronchial secretions, …etc.
◊ Contraindications: hypersensitivity, breast-feeding, children <2 years
of age, …etc.
• H1 antagonists also competes with histamine for H1-receptor sites on
effector cells in the gastrointestinal tract and blood vessels.
• May be used for motion sickness (30 to 60 minutes before motion).
Cardiovascular and renal drugs
◊ Diuretics
◊ Angiotensin-converting enzyme inhibitors
◊ Angiotensin receptor blockers
◊ Calcium channel blockers
◊ Adrenergic antagonists
◊ Direct vasodilators
◊ Cardiac glycosides e.g., digoxin
◊ Vasoconstrictors or vasopressors e.g., dobutamine, epinephrine, …
◊ Potassium channel blockers, e.g., Amiodarone
◊ Antianemic drugs (vitamin B12, folic acid, iron salts)

Diuretics #1
◊ Diuretics is an agent that increases urine output.
◊ Mechanism of action: diminish electrolyte (sodium, chloride,
potassium, …) and water reabsorption at different sites in the
nephron, thereby increasing urinary electrolyte and water losses.
◊ Major clinical indications: edema, heart failure and hypertension.
◊ Types of diuretics and their main site of action:
◊ Loop diuretics act in the thick ascending limb of the loop of Henle
◊ Thiazide-type diuretics in the distal convoluted tubule
◊ Potassium-sparing diuretics in the aldosterone-sensitive distal
nephron (including the connecting tubule and collecting duct)
◊ Potassium sparing diuretics act at collecting tubules.
◊ Carbonic anhydrase inhibitors act in the proximal tubule.

Diuretics #2
1. Thiazides: hydrochlorothiazide, chlorothiazide, …
◊ Action: decrease reabsorption of sodium and chloride in the distal
convoluted tubule by inhibiting the Na-Cl cotransporter.
◊ And also increased excretion of potassium and hydrogen ions.
◊ Clinical use: hypertension, congestive heart failure, nephrolithiasis
(calcium stones), nephrogenic diabetes insipidus, …etc.
◊ Adverse effect: hypersensitivity reactions, hypotension, electrolyte
imbalances (e.g., hyponatremia, hypokalemia, hypochloremia),
hyperglycemia, hyperuricemia, hypercalcemia, photosensitivity, …
◊ Contraindications: known sensitivity, anuria (because they works
efficiently only when urine flow is adequate).
◊ Drug interactions and cautions: digoxin (↑ toxicity due to
electrolyte disturbances), beta-blockers (increase risk of
hyperglycemia), …

Diuretics #3
2. Loop diuretics: e.g., furosemide (lasix), torsemide, …etc.
◊ Action: Na+/K+/2Cl−transporter inhibition.
◊ Inhibit Na+ and Cl- in the thick ascending limb of loop of Henle.
◊ ↓ positive potential.
◊ ↓ reabsorption of K+, Ca2+ and Mg2+.
◊ ↑ diuresis.
◊ Clinical use: ascites due to cirrhosis, heart failure, hypertension, …
◊ Adverse effects: fluid and electrolyte imbalances (e.g.,
hyponatremia, hypokalemia, fluid volume deficit), ototoxicity, …
◊ Contraindications: known sensitivity, anuria, drug interaction, …
◊ Drug interaction: corticosteroids and digoxin (increase the risk of
hypokalemia), aminoglycosides and cephalosporins (increase the
risk of nephrotoxicity, ototoxicity), …etc.

Diuretics #4
3. Potassium-sparing diuretics: spironolactone, amiloride, …
◊ Action: spironolactone is aldosterone receptor antagonist.
◊ Competes with aldosterone for receptor sites in the distal renal
tubules (blocks the sodium-retaining effects of aldosterone),
increasing sodium, chloride and water excretion while conserving
potassium and hydrogen ions.
◊ Clinical use: hyperaldosteronism, adjunct to K+ wasting diuretics,
antiandrogenic uses (female hirsutism), congestive heart failure,
hypertension, hypokalemia, ascites due to cirrhosis, …etc.
◊ Side effects: hyperkalemia, acidosis, antiandrogen, …etc.
◊ Contraindication: hypersensitivity, renal insufficiency (cause
hyperkalemia).
◊ Drug interaction: angiotensin-converting enzyme inhibitors,
angiotensin II receptor blockers, potassium containing drugs
(increase risk of hyperkalemia), …etc.
Diuretics #5
4. Osmotic diuretics, e.g., mannitol
◊ Action:
◊ Increase osmotic pressure causes water to be pulled from
extravascular sites into the bloodstream.
◊ Decrease reabsorption of water and electrolytes in the renal
tubules.
◊ Increases urine volume.
◊ Clinical uses:
◊ ↓ intraocular pressure in glaucoma
◊ ↓ intracranial pressure (cerebral edema, trauma, stroke, …)
◊ Side effects: acute hypovolemia, electrolyte disturbance, …etc.
◊ Contraindication: hypersensitivity.

Diuretics #6
5. Carbonic anhydrase inhibitors e.g., Acetazolamide.
◊ Mechanism of action: reversible inhibition of the enzyme carbonic
anhydrase resulting in reduction of hydrogen ion secretion at renal
tubule and an increased renal excretion of sodium, potassium,
bicarbonate and water.
◊ And also, decreases production of aqueous humor and inhibits
carbonic anhydrase in central nervous system to retard
abnormal and excessive discharge from CNS neurons.
◊ Clinical use: glaucoma, acute mountain sickness, metabolic alkalosis,
…etc.
◊ Side effects: bicarbonaturia, acidosis, hypokalemia, paresthesia,
hyperchloremia, renal stones, …etc.
◊ Contraindication: hypersensitivity to acetazolamide and
sulfonamides, hepatic disease or insufficiency, decreased sodium
and/or potassium levels, adrenocortical insufficiency, cirrhosis, …
Diuretics #7
Nursing implication:
◊ Assess fluid status throughout therapy.
◊ Weight, intake and output ratios.
◊ Amount and location of edema.
◊ Skin turgor and mucous membranes.
◊ Assess for signs of electrolyte imbalance:
◊ Anorexia, muscle weakness, numbness, tingling, paresthesia,
confusion, excessive thirst, …etc.
◊ Monitor BP and pulse before and during administration.
◊ Lab test considerations: electrolytes (especially potassium), blood
glucose, BUN and serum uric acid levels before and periodically
throughout course of therapy.

Diuretics #9
Control question
1. Loop diuretics inhibits sodium and water reabsorption at which

part of the renal anatomy?
A. Early collecting duct
B. Thin ascending loop
C. Thin descending loop
D. Thick ascending loop

Angiotensin converting enzyme inhibitors
◊ Drugs: enalapril, captopril, …
◊ Mechanism of action:
◊ Competitive inhibitor of angiotensin-converting enzyme (ACE).
◊ ACEIs blocks the conversion of angiotensin I to angiotensin II.
◊ Angiotensin II is a potent vasoconstrictor.
◊ Also stimulates aldosterone secretion by adrenal cortex.
◊ Promotes vasodilation (decreasing blood pressure).
◊ ↓ aldosterone secretion (↑ serum k+ and ↓ Na+ & H2O retention).
◊ Clinical use: hypertension, heart failure, …etc.
◊ Side effects: cough, hypotension, acute renal failure (increase BUN and
serum creatinine, resulting in oliguria), hyperkalemia, angioedema, …
◊ Contraindication: hypersensitivity, significant drug interactions, …etc.

The renin–angiotensin–aldosterone pathway

Angiotensin II - receptor blockers (ARBs)
◊ Drugs: losartan, candesartan, valsartan, ...
◊ Mechanism of action: block vasoconstrictor and aldosterone-

secreting effects on angiotensin II by selectively blocking the binding
of angiotensin II to specific tissue receptors in vascular smooth
muscle and the adrenal gland, causing vasodilation and a decrease in
aldosterone effects.
◊ Clinical use: hypertension, heart failure, …etc.
◊ Side effects: hypotension, acute renal failure (increase serum

creatinine)), hyperkalemia, dizziness, cough, hepatitis, …etc.
◊ Contraindication: hypersensitivity, significant drug interactions, …

Calcium channel blockers (CCBs)
◊ Mechanism of action: inhibit the L-type calcium channel on cells.
◊ There are two major categories of CCBs:
◊ Dihydropyridines: predominantly vasodilators.
◊ E.g., nifedipine, felodipine, amlodipine, …etc.
◊ Clinical use: hypertension, angina, …etc.
◊ Non-dihydropyridines: slow cardiac contractility & conduction.
◊ E.g., verapamil and diltiazem.
◊ Clinical use: hypertension, angina, cardiac arrhythmias, …etc.
◊ Adverse effect:
◊ Dihydropyridines: headache, lightheadedness, flushing, …etc.
◊ Non-dihydropyridines: constipation, bradycardia, …etc.
◊ Contraindication: hypersensitivity, cardiogenic shock, hypotension, …

Beta-adrenergic blocking agents
◊ Drugs: propranolol, metoprolol, atenolol, …
◊ Mechanism of action: competitively blocks response to beta1 and
beta2 adrenergic stimulation which results in decreases in heart rate,
myocardial contractility, blood pressure & myocardial oxygen demand.
◊ By occupying beta-receptor sites, they prevents epinephrine or
norepinephrine from exerting their effects.
◊ Clinical use: hypertension, angina, atrial fibrillation, heart attack, …
◊ Side effects: bronchospasm, bradyarrhythmia, CNS effects (fatigue,
insomnia, vivid dreams, memory impairment, erectile dysfunction),
hypoglycemia, … etc.
◊ Contraindication: bradycardia, heart failure, asthma, shock, …
◊ Sudden withdrawal may exacerbate angina & myocardial infarction.

Alpha adrenergic agonist
◊ Drugs: carvedilol, labetalol, …etc.
◊ Mechanism of action: decrease sympathetic impulse from CNS to heart

(reduction of cardiac output, vasodilation, decreased vascular
resistance, reduced plasma renin activity, … etc.).
◊ Clinical use: hypertension, myocardial infarction, angina, atrial

fibrillation, heart failure with reduced ejection fraction, …etc.
◊ Adverse effect: bradyarrhythmia, bronchospasm, CNS effect (fatigue,

sleep disorder, insomnia, and vivid dreams), hypoglycemia, …
◊ Contraindication: serious hypersensitivity, bronchial asthma, severe

bradycardia, cardiogenic shock, severe hepatic impairment, …etc.
Direct acting vasodilators
◊ Drugs acting through nitric oxide: hydralazine, nitroprusside, …etc.
◊ Mechanism of action: direct vasodilation of arterioles (with little
effect on veins) with decreased systemic resistance.
◊ Arterial vasodilation may occur via
◊ Inhibition of calcium release from the sarcoplasmic reticulum.
◊ Inhibition of myosin phosphorylation in arterial smooth muscle.
◊ Clinical use: hypertension, heart failure with reduced ejection
fraction, …etc.
◊ Adverse effect: lupus-like syndrome (hepatosplenomegaly, severe
malaise or myalgias, acute joint pain and swelling, leukopenia,
thrombocytopenia, …), elevated erythrocyte sedimentation rate, …
◊ Contraindication: hypersensitivity, mitral valve rheumatic heart
disease, systemic lupus erythematosus, thyrotoxicosis, …etc.

Mechanism of action of renal and cardiac drugs

Cardiac glycosides
◊ Drugs: digoxin.
◊ Mechanism of action:
◊ Improves the contractility and pumping ability of the heart.
◊ Increases the force of myocardial contractility by inhibiting Na+,
K+, ATP (Na, K-ATPase), an enzyme in cardiac cell membranes
that decreases the movement of sodium out of myocardial cells
after contraction.
◊ As a result, calcium enters the cell in exchange for sodium,
causing additional calcium to be released from intracellular
binding sites and increasing myocardial contractility.
◊ Clinical use: atrial fibrillation, heart failure with reduced ejection
fraction, supraventricular tachycardia, …etc.
◊ Adverse effect: nausea, vomiting, visual disturbances (yellow or
blurred vision), dizziness, hallucination, cardiac arrhythmia, …etc.
Antianemic
◊ Antianemic is a drug used for prevention and treatment of anemia.
◊ Drugs: iron, vitamin B12, folic acid, …etc.
◊ Iron (e.g., ferrous fumarate, ferrous gluconate, ferrous sulfate,
iron dextran, iron sucrose, … etc.) is required for production of
hemoglobin, which is necessary for oxygen transport to cells.
◊ Vitamin B12 and folic acid are water-soluble vitamins that are
required for blood cell production and cell replication (folic acid
is also necessary for purine and pyrimidine synthesis).
◊ Contraindications: undiagnosed anemias, hemochromatosis,
hemosiderosis, hemolytic anemia (iron), …etc.
◊ Drug interaction:
◊ Oral iron ↓ the absorption of tetracyclines and fluoroquinolones.
◊ Phenytoin & other anticonvulsants ↓ the absorption of folic acid.

Drug for diabetes mellitus #1
1. Insulin: lower blood glucose (regulate glucose metabolism):
◊ By stimulating peripheral uptakes.
◊ By inhibiting hepatic glucose production.
◊ Increase glycogen synthesis (convert glucose to glycogen).
◊ By inhibit lipolysis and proteolysis.
◊ Enhance protein synthesis (convert amino acid to protein).
◊ Stimulates triglyceride formation (from free fatty acids).
◊ Target organs for insulin: liver, skeletal muscle and adipose tissue.
◊ Classification of insulin, based on onset and duration of action:
A. Short acting insulin: lispro, aspart and glulisine.
◊ Onset (5 - 15 minutes) and duration of action (4 - 8 hours).
B. Intermediate acting insulin: NPH and Lente.
◊ Onset (1 - 2 hour) and 14 - 24 hours duration of action.
C. Long acting: glargine and Levemir.
◊ 3 to 4 hours onset of action.
◊ > 24 hour duration of action.
◊ Clinical use: type I DM, DKA, …etc.
◊ Adverse effects: hypoglycemia, hypokalemia, …etc.
◊ Contraindication: during episodes of hypoglycemia, …etc.
• Insulin increases cellular permeability to several ions, including

potassium, magnesium and phosphate.
• By activating sodium-potassium ATPases, insulin promotes the
intracellular movement of potassium.

2. Biguanide: metformin
◊ Action: decreases hepatic glucose production, decrease intestinal
absorption of glucose and improves insulin sensitivity (increases
peripheral glucose uptake and utilization)
◊ Clinical use: type 2 DM, …etc.
◊ Adverse effect: GI upset (vomiting, diarrhea, pain, dyspepsia,

flatulence), lactic acidosis, vitamin B12 deficiency, …etc.
◊ Contraindication: hypersensitivity, severe renal dysfunction (GFR

<30 mL/minute/1.73 m2), acute or chronic metabolic acidosis with
or without coma (including diabetic ketoacidosis), …etc.
Insulin, glucagon, and blood glucose
Islets of langerhans in
pancreas:
• Alpha cell: secret
glucagon (raise
blood glucose
level).
• Beta cell: secret
insulin (lower
blood glucose
level).

Pregnancy drug category or classification
◊ Based on the teratogenic and fetotoxic effects, drugs are classified as:
A. Controlled studies show no risk to the fetus.
B. No evidence of risk in human, but negative animal findings.
C. Risk cannot be ruled out.
D. Positive evidence of risk.
E. or X contraindicated in pregnancy.

Assignment need to be submitted, 20 %
Group - 1:
1. The age-related changes in pharmacokinetics (ADME).
2. Antimicrobials that should be avoided in pregnancy and their effect.
Group – 2:
1. Disinfectants and antiseptic agents
Group – 3: • Definition
1. Antidepressant • Mechanism of action
Group – 4: • Clinical use
1. Anticonvulsant • Adverse effect
Group – 5:
1. Common cancer chemotherapy

Thank you !!!
 Any experience is good experience !
Berhanu Wale (BSc and MSc)
Contact me via
4/14/2024

Medication Administeration Part II

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Anti - inflammatory drugs #1

◊ Inﬂammation is a reaction to tissue injury caused by the release of

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◊ Drugs for nausea and vomiting

◊ Drugs for constipation

◊ Drugs for diarrhea

◊ Drugs for inflammatory diseases

◊ Drugs for hemorrhoid

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◊ Includes: Ondansetron, dolasetron, palonosetron, … etc.

◊ Mechanism of action: blocks serotonin, both peripherally on vagal

◊ Adverse effect: constipation, intestinal obstruction, headache, … etc

◊ Contraindication: hypersensitivity, QT prolongation, … etc.

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◊ Scopolamine (hyoscine) = hydrobromide and butylbromide.

◊ Blocks the activity of the muscarinic acetylcholine receptor.

◊ Also, dries secretions, antagonizes histamine and serotonin.

◊ Indication: motion sickness and postoperative.

◊ Sometimes used before surgery to decrease saliva.

◊ Side effect: blurred vision, dilated pupils, dry mouth, sedation, …

◊ Contraindication: hypersensitivity, narrow angle glaucoma, bowel or

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• Coartem is a coformulation of artemether and lumefantrine with

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Reading assignment: diethylcarbamazine, levamisole, …

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• Reading assignment: iodoquinol and pentamidine.

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Drug Primary receptor subtype Primary use

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◊ Mast cell stabilizers

◊ Antitussive, expectorant and mucolytics.

◊ Mechanism of action: relaxes smooth muscle of bronchi and

◊ Clinical use: asthma (acute exacerbation), bronchospasm due to

◊ Adverse effects: tremor, cardiac stimulation (angina, tachycardia and

◊ Contraindications: hypersensitivity, cardiac tachydysrhythmias, ...

◊ Caution: hypertension, hyperthyroidism, diabetes mellitus, ...

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1. Loop diuretics inhibits sodium and water reabsorption at which

B. Thin ascending loop

C. Thin descending loop

D. Thick ascending loop

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