Anti HTN

Question 1

Direct Renin Inhibitors

Answer 1

Aliskerin

inhibit angiotensinogen activation

Diarrhea & Hyperkalemia

Question 2

ACEIs - pril

Answer 2

Enalapril - Lisinopril - Captopril

MoA: inhibit angiotensin I to II

PK: oral - hepatic metabolism - renal excretion - bradykinin

Uses: Hypertension(w/diabetes), HF, and Post MI

ADR: Dry cough, HyperK+, 1st dose HTN

Contra: pregnancy & breastfeeding, Bilateral RAS, Hereditary angioedema

DDI: Spironolactone, K+ supp. & sparing diuretics, ARBs & DRIs

Question 3

ARBs - sartan

Answer 3

Losartan - Candesartan - Irbesartan
MoA: inhibit binding to AT1 receptor

PK: significant hepatic elimination, no bradyknin

Uses: HTN(w/diabetes & CKD) & HF

ADR: like ACEIs (less dry cough & angioedema)

Contra: Pregnancy

DDIs: ACEIs & DRIs

Question 4

CCBs (Dihydropyridines) - dipine

Answer 4

Amlodipine & Nifedipine
(on Periphery)

MoA:↓Ca2+ into vascular SM

PK: oral, short half-lives (3-8hrs), Amlodipine (40-60hrs), sustained release

Uses: HTN, Angina, Raynaud’s

ADR & Contra: Flushing, Headache, Pretibial swelling

DDIs: Nitrates

Question 5

CCBs (Non-Dihydropyridines)

Answer 5

Verapamil (V) & Diltiazem (D)
(on Myocardium)

MoA: reduce Ca2+ into vascular SM

PK: oral, short half lives (3-8hrs), sustained release

Uses: HTN, Angina, Arrhythmia

ADR & Contra: Hypotension, Bradycardia, HF, Constipation (V), Pretibial swelling (D)

DDIs: Beta blockers & Digoxin

Question 6

Thiazide & Thiazide like Diuretics -Thiazide

Answer 6

Bendroflumethiazide, Hydrochlorothiazide, Indapamide, Chlorthalidone
MoA: (-) of Na+/Cl- transporter @DCT

PK: oral, 1-3week to stabilize BP, long half-lives (6-12hrs)

Uses: HTN, HF, Hypercalciuria

ADR: Hypo(tension - natremia - kalemia)
Hyper(glycemia - calcemia - uricemia)

Question 7

K+ Sparing Diuretics -one

Answer 7

Epithelial Na+ channel blockers:
Amiloride & Triamterene
Aldosterone antagonists:
Eplerenone & Spironolactone

MoA: ↓K+ & ↑Na+ excretion

Uses: 2ry Hyperaldosteronism(liver cirrhosis & nephrotic syndrome), HF, Resistant HTN, Ascites

ADR: Hyperkalemia, Gynecomastia (E&S), Menstrual irregularities (S)

DDIs: Digoxin, ACEIs (hyperkalemia)

Question 8

Loop Diuretics -ide

Answer 8

Bumetanide - Furosemide

MoA: ↑ excretion of Na+ , K+ , Ca2+

ADR:
Hypo(tension-natremia-kalemia-calcemia)
Hyperglycemia

Question 9

Beta blockers -lol

Answer 9

Atenolol (β1) - Propranolol(β1&2) - Labetalol (α&β)

MoA: ↓activation of β1 adrenoreceptors

PK: oral, takes several weeks, extensive 1st-pass metabolism (P)

Uses: Angina(post MI), HF, AF, HTN, Thyrotoxicosis, Anxiety, Tremor

ADR: Bronchoconstriction, Bradycardia, Sleep disturbances, ED, NODM

Contra: Uncontrolled HF, Asthma

DDIs: Verapamil (severe bradycardia)

Abrupt Withdrawal: Angina & MI in IHD patients

Question 10

α-1 blockers -zosin

Answer 10

Prazosin - Doxazosin
MoA: block α-1 receptors↓intracellular calcium conc.
Uses: HTN w/ pheochromocytoma, as adjunct in BPH, last resort
ADR: Postural hypotension
DDIs: Hypotensive drugs
Abrupt Withdrawal: rebound hypertension

Question 11

Centrally Acting Drugs (alpha-2 agonists)

Answer 11

MoA: inhibit norepinephrine release

Clonidine
PK: oral/transdermal patch, excreted by kidney
Uses: HTN(unresponsive or w/renal disease)
ADR: Sedation, Bradycardia
Abrupt Withdrawal: Rebound HTN

Methyldopa
Uses: HTN in pregnancy
ADR: Sedation, Drowsiness limited use