Antihypertensive Drugs and their use in Management of Essential HTN Flashcards
What are the ACE inhibitors?
- Captopril
- Lisinopril
- Enalapril (pro-drug)
- Ramipril (pro-drug)
What are some AT1-receptor blockers?
- Losartan (pro-drug)
- Valsartan
- Iresartan
- Telmisaratan
- Candesartan
What is a renin inhibitor?
Aliskerin
What are some dihydropyridine Ca2+ channel blockers?
- Amoldipine
- Nifedipine
- Nicardipine
- Nimodipine
What are some direct vasodilators?
- Minoxidil
- Na-Nitroprusside
- Hydralazine
- Fenaldopam
What is hypertensive treatment indicated in a patient 60y/o+? JNC 8
SBP over 150 or
DBP over 90
goal is less than these numbers
What is hypertensive treatment indicated in a patient less than 60y/o?
DBP over 90 or SBP over 140. Grade A (age 30-59)
What are the main effects of Prazosin?
decrease TPR and reduce BP by blocking a1 receptors on arteries and veins
What are the main effects of Doxazosin and Terazosin?
relieve symptoms of BPH by relaxing the muscles of the bladder and prostate
not great anti-HTN agents
Side effects of a-blockers?
first dose hypotension (give at bedtime)
Are a-blockers first-line for HTN?
No, mostly due to results of the ALLHAT study which showed that they increased CHF risk in patients with HTN.
mostly used for BPH now
What are some 3rd generation B-blockers with a and B activities?
- Labetalol
- Carvedilol
- Nebivolol
What receptors does Labetalol inhibit?
non-selective B (B1/B2) and a1
What is Labetalol given for?
IV for HTN emergency (pheochromocytoma and preeclampsia)
What are some functions of Carvedilol?
mixed a1-B antagonist with:
- antioxidant (binds and scavenges ROS)
- protects membranes from lipid peroxidation (prevents LDL oxidation and uptake into arteries)
What are some functions of Nebivolol?
B1 selective antagonist with NO-mediated vasodilation and Antioxidant activity
What is the MOA of BB without ISA?
they block myocardial B1 receptors leading to decreased HR and contractility and
block juxtaglomerular B1 receptors, inhibiting renin release
Do BB cause retention of salt and water?
No, can be administered without a diuretic. (however, more effective with one)
Are BB designed for first line use for HTN?
No, if necessary it is preferable to use 3rd generation (causes increase stroke risk) as per JNC 8
Indications for BB?
- Hypertensive patients with conditions such as MI, IHD, or CHF (carvedilol and metoprolol XL are cardio protective in these patients and tend to increase SV)
- Hypertensive patients with hyperthyroidism and migraines
- prevent subsequent MI
- HTN with high renin
What BB is used in open angle glaucoma treatment?
Timolol (reduces production of aqueous humor)
What else can BB be used for?
- stage fright
- altering memory
- sinus and AV arrhythmias
What are some side effects of 1st/2nd generation BBs?
-poor perfusion to extremities (due to a1 mediated vasoconstriction when the sympathetic system is activated following decreased BP)
- bradycardia
- bronchospasm
- bad dreams, depression
- metabolic effects
T or F. ALL BB should be avoided in asthma
T. (B1/3rd generation are okay in patients with COPD)
What are some of the metabolic effects of BB?
- block glycogeneolysis
- delay recovery from hypoglycemia in type I diabetes (mask tachycardia)
- block HSL in adipocytes - increase LDL and TAG
- reduce HDL
How can the delay recovery from hypoglycemia in type I diabetes seen in BB be avoided?
not seen in 3rd ben or with selective B1-blockers
Is it safe to withdraw BB use suddenly?
no, prolonged use up-regulates B-receptors in the heart. Abrupt withdrawal causes tachycardia
taper 10-14 days prior
What do ACEIs do?
- inhibit conversion of angio I to II
- inhibit bradykinin breakdown, a vasodilator
- slightly decrease aldosterone levels
increase renal BF (dilate renal artery) without an increase in GFR and increase synthesis of prostaglandins
What does the increase in Prostaglandins via ACEIs do?
delay progression of renal disease in diabetics (renoprotective)
What are the effects of Angiotensin II?
- cardiac and vascular hypertrophy (via PKC activation)
- systemic vasoconstriction
- increased thirst
- stimulates aldosterone release from the adrenal cortex
- stimulates ADH release from the pituitary leading to renal sodium and fluid retention