Antihypertensives Flashcards
Which drug can be used for opiate, ethanol and smoking withdrawal?
Clonidine
How to alpha 2 agonists (clonidine and methyldopa) treat hypertension?
Agonize presynaptic alpha 2 receptors in the CNS to decrease sympathetic output, which decreases TPR and HR
Side effects of A2 agonists
Sedation
Depression (clonidine more severe)
Postural hypotension
Edema (due to hypotension inducing activation of renin-angiotensin-aldosterone)
Coombs test positive-hemolytic anemia- methyldopa
Dry mouth (clonidine)
Major side effect of methyldopa
Coombs test positive-hemolytic anemia
How do TCAs affect A2 agonists?
TCAs decrease the effects of A2 agonists
What can occur if you suddenly stop taking clonidine?
Hypertension crisis
Reserpine MOA
Reserpine: inhibits vesicular membrane-associated transporter (VMAT), prevents dopamine and norepinephrine vesicle uptake, depletes norepinephrine in nerve terminal vesicles
Does reserpine cross the BBB?
Yes
Side effects of reserpine
Depression (decrease NE, serotonin in CNS)
Diarrhea
Increase gastric acid secretion
Contraindications for reserpine
Depression
History of peptic ulcers
Guanethidine MOA
Taken up by NET and replaces norepinephrine from vesicle, cytosolic NE then is degraded by MAO—depleting NE in vesicle
Inhibits vesicle fusion with membrane, inhibits vesicular norepinephrine release
Does guanethidine cross the BBB?
NO
Side effects of guanethidine
Orthostatic hypotension
Diarrhea
Edema
Sexual dysfunction (delayed or retrograde ejaculation)
Which drugs can cause hyperlipidemia?
B blockers
Which drug dilates both arteries and veins?
Nitroprusside
Hydralazine MOA
Acts through the release of NO and mainly dilates the artery
What is a major ADR of hydralazine?
Drug-induced reversible lupus (SLE) like syndrome (especially in people who are slow acetylators)
Nitroprusside MOA
MOA: release of NO from the drug molecule (NO donor), this stimulates guanylyl cyclase and increases cGMP in smooth muscle.
What is a major ADR of nitroprusside?
Cyanide poisoning
MOA of diazoxide and minoxidil
Potassium channel opening drugs
Induce hyperpolarization—leading to arterial vasodilation
What else can diazoxide be used for?
To treat insulinoma because it reduces insulin
Side effects of potassium channel opening drugs
Decrease insulin (diazoxide, treat insulinoma),
Hypertrichosis (minoxidil)
Hypotension
Salt and water retention
Which drugs are ACEIs?
Catopril, enalapril, lisinopril
Which drugs are angiotensin receptor blockers?
Losartan, valsartan
MOA of Aliskiren
Renin inhibitor. Not as effective as ACEIs.
Major ADR of RAAS drugs
Hyperkalemia, should not be used with potassium sparing diuretics
ADR of ACEIs
Cause accumulation of bradykinin –> dry cough
Rare: angioedema
When should RAAS drugs not be used?
Bilateral renal artery stenosis because they can cause renal failure
PREGNANCY –> can cause craniofacial abnormalities and renal dysgenesis in the fetus
First choice for diabetic nephropathy
ACEIs (dilate efferent artery of the glomerulus ad decrease GFR –> delays deterioration of kidney function)
Which is constricted more by angiotensin II: afferent or efferent?
Efferent
Main drugs to remember for treatment of hypertensive crisis
Nitroprusside/nitroglycerin
Diazoxide
Fenoldopam
Lebetalol
Stage I HTN treatment in non black people
Monotherapy
thiazide, ACEI, ARB, CCB
Stage I HTN treatment in black people
Thiazide, CCB
Treatment for patients with HTN and diabetes or kidney disease
ACEI, ARB (delay deterioration of kidney)
Treatment choice for heart failure
ACEI/ARB + BB + diuretic + spironolactone
Treatment choice for post-MI
ACEI/ARB and BB
Treatment choice for coronary artery disease
ACEI, BB, diuretic, CCB
Treatment choice for diabetes
ACEI/ARB, CCB, diuretic
Treatment choice for chronic kidney disease
ACEI/ARB
Treatment choice for recurrent stroke
ACEI, diuretic
Treatment choice for thoracic aortic disease
BB
Treatment choice for pregnancy
Labetolol, nifedipine, methyldopa