Pharmacology
Antiglaucoma Drugs
Antiglaucoma drugs aim to manage intraocular pressure, preventing optic nerve damage in glaucoma. They include beta-blockers, prostaglandin analogs, alpha agonists, carbonic anhydrase inhibitors, and miotic agents. Each class targets different mechanisms to reduce intraocular pressure and preserve vision. …
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Pharmacology
Allopurinol
Class: Xanthine Oxidase Inhibitor; Antigout Dosage Forms. Tablet: 100 mg, 200 mg, 300 mg MOA. Allopurinol decreases the production of uric acid by inhibiting the action of xanthine oxidase, the enzyme that converts hypoxanthine to xanthine and xanthine to uric acid. …
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Pharmacology
5∝-reductase inhibitors
5∝-REDUCTASE INIHIBITORS... EXAMPLES: Dutasteride, finasteride. MECHANISM OF ACTION: Competitively inhibit the metabolism of testosterone to dihydrotestosterone (a more potent androgen) in peripheral tissues. Reduced circulating dihydrotestosterone leads to reduced prostatic volume and thereby relief of voiding symptoms. INDICATIONS Beni…
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Pharmacology
Aminoglycosides
AMINOGLYCOSIDES ANTIBIOTICS... EXAMPLES: Gentamicin, tobramycin, amikacin, neomycin, streptomycin. MECHANISM OF ACTION: Bacteriocidal antibiotic that blocks protein synthesis by binding to the bacterial 30S ribosomal subunit. This prevents the process of tRNA attachment and mRNA translation is disrupted. INDICATIONS Septicae…
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Pharmacology
Aciclovir
ACICLOVIR ANTI-VIRAL... MECHANISM OF ACTION: Synthetic analogue of guanosine, which is phosphorylated to become an active compound, aciclovir triphosphate. Aciclovir triphosphate competes with the natural nucleotide as a substrate to viral DNA polymerase and thus inhibits viral DNA replication. INDICATIONS Treatment and prophylaxis of h…
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Pharmacology
Antihistamine anti-emetics
ANTIHISTAMINE ANTIEMETICS... EXAMPLES: Cyclizine, promethazine. MECHANISM OF ACTION: H1 receptor antagonists directly inhibit the CTZ in the medulla. They possess anticholinergic and anti-emetic properties. Cyclizine also increases lower oesophageal sphincter tone and reduces the sensitivity of the labyrinthine apparatus. IND…
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Pharmacology
5-HT3 antagonists
5-HT3 ANTAGONIST... EXAMPLES: Ondansetron, granisetron. MECHANISMOF ACTION: Selective 5-HT3 receptor antagonists that act peripherally on vagal nerve endings of the GI tract and centrally in the CTZ. 5-HT3 receptors in the CTZ in the area postrema of the medulla contribute to the perception of nausea and the control of vomiting. INDICATIO…
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Pharmacology
5-HT1 agonists (triptans)
5-HT1 AGONIST (TRIPTANS)... EXAMPLES: Sumatriptan, zolmitriptan. MECHANISM OF ACTION: Selective activation of 5-HT1 receptors that are predominantly located in cranial blood vessel walls. 5-HT1 receptors mediate vasoconstriction thereby relieving symptoms that are believed to result from the dilatation of intra- and extracranial vessels. …
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PPIs
Proton pump inhibitors (PPIs)
PROTON PUMP INHIBITORS... EXAMPLES: Omeprazole, lansoprazole, esomeprazole, pantoprazole. MECHANISM OF ACTION: Inhibit H + /K + ATPase on luminal surface of gastric parietal cells and thereby reduce gastric acid secretion. INDICATIONS Gastric/duodenal ulceration. As part of triple therapy for eradication of Helicoba…
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Pharmacology
Laxatives
LAXATIVES... EXAMPLES: Lactulose, Egycosate. MECHANISM OF ACTION: Bulk laxatives (e.g. ispaghula husk) – polysaccharide polymers that are not broken down by digestion and thereby increase stool volume. This stimulates intestinal peristalsis (via the stretch reflex) as well as softening faeces. Osmotic laxatives (e.g. lactulose, Movicol) – these poorly absorbed so…
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Pharmacology
𝛃2 adrenoceptor agonists
𝛃2 ADRENOCEPTOR AGONIST... EXAMPLES: Short-acting – salbutamol, terbutaline; long-acting – salmeterol, formoterol. MECHANISM OF ACTION: Selective 𝛃2 adrenoceptor agonists in smooth muscle of upper airways that increase intracellular cAMP. This leads to smooth muscle relaxation and bronchodilation. INDICATIONS Acute asthma …
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Pharmacology
Aldosterone antagonists
ALDOSTERONE ANTAGONIST... EXAMPLES: Spironolactone, eplerenone. MECHANISM OF ACTION: Competitive antagonist at intracellular aldosterone receptors in renal tubules causing reduced production of aldosterone-induced proteins. This indirectly reduces activity of Na/K ATPase in the collecting ducts, increasing excretion of sodium and decreasing potassium loss. Spironolac…
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Pharmacology
𝝰-adrenoceptor antagonists (𝝰 blockers)
𝝰-ADRENOCEPTOR ANTAGONISTS (𝝰 blockers)... EXAMPLES: Doxazosin, prazosin, tamsulosin, alfuzosin. MECHANISM OF ACTION: Inhibit 𝝰 1-adrenoceptors in arterioles, thereby reducing tone of vascular smooth muscle and reducing total peripheral resistance. Inhibition of 𝝰1-adrenoceptors in periurethral prostatic stroma results in relaxation of internal urethral sphinct…
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Pharmacology
Histamine type 2 receptor antagonists
HISTAMINE TYPE 2 RECEPTOR ANTAGONISTS... EXAMPLES: Ranitidine, cimetidine. MECHANISM OF ACTION: Competitive inhibitors of all histamine type 2 receptors. Inhibit histamine- and gastrin-stimulated gastric acid secretion by their action on parietal cells in the stomach. INDICATIONS Gastric and duodenal ulcers. Gastro-oesophageal reflux…
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Pharmacology
Ferrous sulfate
Oral (30% elemental iron) , indicated for treatment & prevention iron deficiency anemia . Action ㅡ an essential mineral found in hemoglobin, myoglobin, and many enzymes. Enters the bloodstream and is transported to the organs of the reticuloendothelial system (liver, spleen, bone marrow) where it becomes part of iron stores. Therapeutic effects ㅡ resolution o…
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Pharmacology
Naproxen
Analgesic, NSAID (nonopioid), anti-inflammatory and antirheumatic approved as an over-the-counter (OTC) medication in 1994. For further information, see topic on Recommendations for safety use of NSAIDs . Mechanism of Action ㅡ Naproxen blocks arachidonate binding to competitively inhibit both cyclooxygenase (COX) isoenzymes, COX-1 and COX-2, resulting in an…
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Pharmacology
Ibuprofen (Brufen, Ibufen)
Analgesic, NSAID (nonopioid), anti-inflammatory, antipyretic and antirheumatic . For further information, see topic on Recommendations for safety use of NSAIDs . Mechanism of Action ㅡ Ibuprofen competitively inhibits both cyclooxygenase (COX) isoenzymes, COX-1 and COX-2, by blocking arachidonate binding resulting in analgesic, antipyretic, and anti-inflammatory ph…
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Pharmacology
Ascorbic acid (Vitamin C)
Vitamin, water soluble. Mechanism of Action ㅡ Ascorbic acid is an essential water soluble vitamin that acts as a cofactor and antioxidant. Ascorbic acid is an electron donor used for collagen hydroxylation, carnitine biosynthesis, and hormone/amino acid biosynthesis. It is required for connective tissue synthesis as well as iron absorption and storage. Sources ㅡ Oran…
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Pharmacology
Aspirin (Aspocid, Ezacard)
Analgesic, NSAID (nonopioid), anti-inflammatory, antiplatelet, antipyretic and antirheumatic. For further information, see topic on Recommendations for safety use of NSAIDs . Mechanism of Action Anti-inflammatory effect, inhibits prostaglandin biosynthesis. Analgesic effect, relieves pain of mild to moderate intensity. Antipyreti…
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