Pharmacology Drug Classes and Mechanisms Summary
NSAIDs: Pain Relief and Inflammation Reduction
NSAIDs (Non-Steroidal Anti-Inflammatory Drugs) are a class of meds that reduce inflammation, pain, and fever. They’re like the ultimate pain relief squad.
Classification
- Non-selective COX inhibitors: Aspirin, Ibuprofen, Diclofenac, Naproxen
- COX-2 selective inhibitors: Celecoxib, Etoricoxib
Pharmacology of Aspirin
- Mechanism: Aspirin irreversibly inhibits COX-1 and COX-2 enzymes, reducing prostaglandin synthesis, which leads to decreased pain, inflammation, and fever.
Anti-Hypertensive Drug Classification
- Diuretics: Thiazides, Loop diuretics, Potassium-sparing
- Beta blockers: e.g., Metoprolol, Atenolol
- ACE inhibitors: e.g., Lisinopril, Enalapril
- Angiotensin receptor blockers (ARBs): e.g., Losartan, Valsartan
- Calcium channel blockers (CCBs): e.g., Amlodipine, Verapamil
- Alpha blockers: e.g., Prazosin
- Vasodilators: e.g., Hydralazine, Minoxidil
Calcium Channel Blockers
- Mechanism of Action (MOA): Block L-type calcium channels in vascular smooth muscle and heart, leading to vasodilation and reduced peripheral resistance.
- Examples: Amlodipine, Verapamil, Nifedipine
Nitrates MOA
- MOA: Release nitric oxide (NO), causing vasodilation (mainly venous), reducing preload and myocardial O2 demand.
Management of Hypertension in Pregnancy
- Mild HTN: Monitor closely, lifestyle changes.
- Moderate to severe HTN:
- First-line: Methyldopa, Labetalol
- Other options: Nifedipine, Hydralazine
- Avoid: ACE inhibitors, ARBs
Drugs Acting on Uterus
- Uterine stimulants (Oxytocics): Oxytocin, Prostaglandins, Ergot alkaloids
- Uterine relaxants (Tocolytics):
- Beta-2 agonists (e.g., Salbutamol)
- Calcium channel blockers (e.g., Nifedipine)
- Oxytocin receptor antagonists (e.g., Atosiban)
Pharmacology of Oxytocin
- MOA: Stimulates oxytocin receptors in uterine muscle, increasing intracellular calcium and uterine contractions.
- Uses:
- Labor induction/augmentation
- Postpartum hemorrhage control
Oral Contraceptives Classification
- Combined Oral Contraceptives (COCs): Estrogen + Progestin (e.g., Ethinyl estradiol + Levonorgestrel)
- Progestin-only Pills (POPs): Only progestin (e.g., Norethindrone)
Pharmacology of COCs
- MOA: Suppress LH/FSH, inhibit ovulation; thicken cervical mucus; alter endometrium.
- Common Uses: Pregnancy prevention, Menstrual regulation, Acne/hirsutism treatment
Oral Hypoglycemic Agents Classification
- Biguanides: e.g., Metformin
- Sulfonylureas: e.g., Glibenclamide, Gimepiride
- Meglitinides: e.g., Repaglinide
- Thiazolidinediones: e.g., Pioglitazone
- DPP-4 inhibitors: e.g., Sitagliptin
- SGLT2 inhibitors: e.g., Dapagliflozin
- Alpha-glucosidase inhibitors: e.g., Acarbose
Pharmacology Highlights (Hypoglycemics)
- Metformin: Decreases hepatic glucose production; increases insulin sensitivity.
- Sulfonylureas: Stimulate insulin release from pancreas.
- DPP-4 inhibitors: Increase incretin levels, enhance insulin secretion.
- SGLT2 inhibitors: Block glucose reabsorption in kidneys, increase glucose excretion.
Autacoids
- Definition: Autacoids are locally acting chemical messengers that have potent biological effects.
- Classification:
- Amine autacoids: Histamine, Serotonin
- Peptide autacoids: Angiotensin, Bradykinin
- Lipid autacoids: Prostaglandins, Leukotrienes
H1 Receptor Antagonists
- Definition: Drugs that block histamine H1 receptors, used mainly for allergies.
- Examples: Diphenhydramine, Loratadine
- Uses: Allergic rhinitis, itching, urticaria, motion sickness
- Effects: Reduce allergic symptoms; 1st gen can cause sedation.
Diuretics Classification
- Thiazide diuretics: e.g., Hydrochlorothiazide
- MOA: Inhibit Na-Cl cotransport in DCT
- Loop diuretics: e.g., Furosemide
- MOA: Inhibit Na-K-2Cl cotransport in Loop of Henle
- Potassium-sparing diuretics: e.g., Spironolactone, Amiloride
- MOA: Block aldosterone or ENaC
- Carbonic anhydrase inhibitors: e.g., Acetazolamide
- MOA: Inhibit CA in PCT
- Osmotic diuretics: e.g., Mannitol
- MOA: Increase osmotic pressure in tubules
Diuretic Pharmacology Highlights
- Thiazides: $\downarrow$BP, $\downarrow$Ca excretion
- Loop diuretics: Potent diuresis, used in edema, acute pulmonary edema
- K-sparing: $\downarrow$K loss, used with other diuretics or in hyperaldosteronism
Arachidonic Acid Pathway
- Arachidonic acid is released from membrane phospholipids by phospholipase A2.
- AA is metabolized via:
- Cyclooxygenase: $\rightarrow$ Prostaglandins, Thromboxanes
- Lipoxygenase: $\rightarrow$ Leukotrienes
- Cytochrome P450: $\rightarrow$ Epoxyeicosatrienoic acids
Prostaglandins
- Physiological roles:
- PGE2: Pain, fever, inflammation; gastric protection
- PGI2: Vasodilation, inhibits platelet aggregation
- TXA2: Vasoconstriction, platelet aggregation
- Psychological roles: Involved in mood regulation, stress response
Bioassay Principles
- Definition: Quantitative measurement of a drug’s potency using biological responses.
- Principle: Compares test drug’s effect with a standard drug on a biological system.
Types of Bioassays
- In vivo: In living organisms
- In vitro: In isolated tissues/cells
- Ex vivo: Tissues from animals
Bioassay Examples
- Insulin:
- Method: Rabbit blood sugar $\downarrow$ or rat diaphragm glucose uptake
- Principle: Insulin’s hypoglycemic effect or glucose uptake in tissues
- Oxytocin:
- Method: Rat uterus contraction or milk ejection in lactating rat
- Principle: Oxytocin stimulates uterine contractions or milk ejection
Anti-Hyperlipidemic Agents
- Definition: Drugs that lower lipid levels in blood.
- Classification:
- Statins: e.g., Atorvastatin
- Fibrates: e.g., Fenofibrate
- Bile acid sequestrants: e.g., Cholestyramine
- Cholesterol absorption inhibitors: e.g., Ezetimibe
- PCSK9 inhibitors: e.g., Alirocumab
HMG-CoA Reductase Inhibitors (Statins)
- MOA: Inhibit HMG-CoA reductase, a key enzyme in cholesterol synthesis in the liver.
- Effect: $\downarrow$Cholesterol synthesis, $\uparrow$LDL receptor expression, $\downarrow$LDL cholesterol.
- Examples: Atorvastatin, Rosuvastatin, Simvastatin
MOA of Statins
- Reduce hepatic cholesterol synthesis.
- $\uparrow$LDL receptor expression $\rightarrow \downarrow$LDL cholesterol in blood.
Thyroid Drugs
- Thyroid hormones: e.g., Levothyroxine, Liothyronine for hypothyroidism.
- Anti-thyroid drugs: e.g., Methimazole, Propylthiouracil for hyperthyroidism.
Thioamides
- MOA: Inhibit thyroid peroxidase, blocking:
- Iodination of tyrosine
- Coupling of iodotyrosines to form T3/T4
- Examples: Methimazole, Propylthiouracil
Drugs for Congestive Heart Failure (CHF)
- Diuretics: e.g., Furosemide
- ACE inhibitors: e.g., Lisinopril
- Beta blockers: e.g., Metoprolol
- ARBs: e.g., Losartan
- ARNIs: e.g., Sacubitril/valsartan
- Inotropes: e.g., Digoxin
Drugs for Angina Pectoris
- Nitrates: e.g., Nitroglycerin
- Beta blockers: e.g., Metoprolol
- Calcium channel blockers: e.g., Amlodipine
- Anti-platelets: e.g., Aspirin
