AntiHTN drugs

Question 1

What are the two A2 agonists talked about and their MOA ?

Answer 1

clonidine methyldopaMOA: decrease sympathetic output, decrease TPR and HR.

Question 2

What are uses for Clonidine and Methlydopa?

Answer 2

Mild or moderate hypertensionClonidine for opiate and ethanol and smoking withdrawalMethyldopa for hypertension in pregnancy

Question 3

Side effects of Clonidine and Methyldopa?

Answer 3

Side effects:Depression (clonidine more severe)Coombs test positive-hemolytic anemia- methyldopaDry mouth (clonidine)Sudden withdrawal—hypertension crisis (clonidine)

Question 4

MOA of reserpine ?

Answer 4

MOA: inhibits vesicular membrane-associated transporter (VMAT) -prevents dopamine and norepinephrine vesicle uptake -depletes norepinephrine in nerve terminal vesicles crosses BBB

Question 5

side effects & contraindications of reserpine?

Answer 5

Side effects: Depression (due to decrease NE, serotonin in CNS) Diarrhea Increase gastric acid secretion Depression Peptic ulcer history

MOA: inhibits vesicular membrane-associated transporter (VMAT) -prevents dopamine and norepinephrine vesicle uptake -depletes norepinephrine in nerve terminal vesicles crosses BBB

Question 6

MOA of guanethidine ?

Answer 6

–up-taken by NET–replaces norepinephrine from vesicle,cytosolic NE then is degraded by MAO—depleting NE in vesicle–inhibitsvesicle fusion with membrane, inhibits vesicularnorepinephrine release.Guanethidine DOES NOT cross BBB

Question 7

Side effects w/ contraindications

Answer 7

–up-taken by NET–replaces norepinephrine from vesicle,cytosolic NE then is degraded by MAO—depleting NE in vesicle–inhibitsvesicle fusion with membrane, inhibits vesicularnorepinephrine release.Guanethidine DOES NOT cross BBB

Side effects:–Orthostatic hypotension–Diarrhea–Edema–Sexual dysfunction (delayed or retrograde ejaculation)Anti hypertension effect can be inhibited by NET blockers (cocaine, tricyclic antidepressants).

Question 8

Alpha blockers

Answer 8

•Blocks irreversiblyα1 andα2:phenoxybenzamine•Blocks reversiblyα1 andα2:phentolamine•Block α1 reversibly:–Prazosin, terazosin,tamsulosin,doxazosin

Question 9

Uses and ADR of Alpha blockers

Answer 9

•Blocks irreversiblyα1 andα2:phenoxybenzamine•Blocks reversiblyα1 andα2:phentolamine•Block α1 reversibly:–Prazosin, terazosin,tamsulosin,doxazosin

Uses:–Unselective α blockers for hypertension emergency by IV–Selective α1 blockers: hypertension + benign prostate hypertrophy•ADR:first dose effect (phenomena)(orthostatic hypotension)– oralα1blockers

Question 10

B receptor blockers MOA

Answer 10

          -decrease CO by decreasing HR, heart contraction, heart conduction-decrease TPR by reducing renin

Question 11

B receptor blockers drugs?

Answer 11

1. Unselective β1 andβ2 receptor blockers:propranolol2. Selectiveβ1 receptor blockers:atenolol, esmolol,metoprolol,3.αandβreceptor blockers:Carvedilol - decreases mortality in patients with HF = increases survival in HFLabetalol- HTN emergency in pregnancy or pheochromocytoma

Question 12

Uses of B blockers:

Answer 12

HTNANGINAMIARRYTHMIASHEART FAILURE

Question 13

ADR of B Blockers:

Answer 13

–Asthma (blockβ2receptor)–Heart block and heart failure–Impaired exercise tolerance–Hyperlipidemia (increase LDL)–Sexual dysfunction–Diabetes (alter hyperglycemia and mask hypoglycemia)

Question 14

Fourmajor mechanisms of vasodilators:

Answer 14

–Blockade of Ca2+ channels–Release of Nitric oxide (NO)–Opening of K+channels-Activation of D1receptors (fenoldopam

Question 15

Calcium channel blockers MOA

Answer 15

Reduce calcium entry into cells, no calcium-calmodulin, no MLCK = SM relaxationdecrease contraction and conduction

Question 16

What are the CCBs?

Answer 16

Dihydropyridine:nifedipine, clevidipineNondihydropyridine:diltiazem,verapamil

Question 17

Hydralazine: acts through the release of whatAND mainly what vessel ?

Answer 17

NOArteries

Question 18

Uses and ADR of hydralazine

Answer 18

•hypertension with pregnancy•ADR: compensatory responses-tachycardia, salt and water retention.•Drug inducedreversible lupus (SLE) like syndrome(especially in people who areslowacetylators).

Question 19

•what are the other two drugs can cause SLE-like syndrome?

Answer 19

Idk

Question 20

What drugs cause Torsades de pointes? (ABCDE)

Answer 20

AntiArrhythmics (class IA, III), 
antiBiotics (eg, macrolides), 
anti“C”ychotics (eg, haloperidol), 
antiDepressants (eg, TCAs), 
antiEmetics (eg, ondansetron) 

(ABCDE)