Kruse - Sympathoplegic Agents Flashcards by Tasfia Ahmed

When are sympathoplegic drugs most effective?

When used with a diuretic

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B-adrenoreceptor antagonists are broken into 4 types

A. Non-selective = Non-ISA (intrinsic sympathomimetic activity) + ISA

B. B1 selective = non-ISA + ISA

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Non-selective b-adrenoreceptor antagonists

Non-ISA = 4 of them (PCNT)

Propranolol
Carvedilol
Nodolol
Timolol

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Non-selective b-adrenoreceptor antagonists

ISA = 4 of them (LCPP)

Labetolol
Cartelol
Penbutolol
Pindolol

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B1-selective b-adrenoreceptor antagonists

ISA = 2 (AN)

Acebutaolol

Nebivolol

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B1 selective b-adrenoreceptor antagonists

Non-ISA = 5 of them (MAEBB)

Metoprolol
Atenolol
Esmolol
Bisoprolol
Betaxolol

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B-adrenergic antagonists are called

B blockers

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B-blockers are useful in preventing

Reflex tachycardia — results from tx with direct vasodilators in severe HTN

also help reduce mortality after MI + heart failure pts

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B-blocker prototype is

Propranolol

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MOA of propranolol

non selective non ISA b-blocker

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What is the effect of B-blockers like propranolol?

decrease bp by decreasing CO
some can vasodilate, but dont cause HTN in healthy normotensive pts
blocking B1 receptors in kidney inhibits renin release
some have local anesthetic effect by blocking Na channels

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All b-blockers are available orally, except

Esmolol

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5 b-blockers avaialble via IV (parental prep) (AELMP)

Atenolol
Esmolol
Labetalol
Metoprolol
Propranolol

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Which 2 b-blockers readily cross BBB?

Why?

Propranolol
Penbutalol

Because they are lipophilic

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Side Effects of B-blockers for asthmatics

blocking B2 receptors in bronchial smooth muscle = constrict ion

** there are no B1 selective agents that completely AVOID b2 receptors

benefits may outweight the risk for COPD patients if they have ischemic heart disease

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Side effects of b-blcokers for diabetics

glycogenolysis inhibited by blocking B2 receptors = can mask hypoglycemia
use with caution for insulin-dependent iabetics

***benefits may outwieght costs in diabetics after MI

Common side effect of b-blockers

Bradycardia
Fatigue
Sexual dysfxn
Depression

Chronic use = can lead to increased VLDL + decreased HDL = BAD!!
Sudden withdrawal can cause: rebound HTN, angina, MI

B-blocker drug-drug interactions

heart block if combined with non-DHP CCBs (verapamil + dilitiazem) — which slow conduction

Clinical uses of b-blockers

HTN
Heart failure
Ischemic Heart disease
Cardiac Arrhythmias
Glaucoma

B-blockers with B1 selectivity can be especially helpful for ppl with

Comorbid asthma
Diabetes
Peripheral vasc. Resistance

B1 blockers with partial B2-agonist activity can be advantageious in patients with

Bradyarrhythmias or peripheral vasc. Disease

Which two b-blockers are widely used for HTN

Metropolol + atenolol

b-blockers will make ACUTE congestive heart failure better or worse?

Worse

Which 4 b-blockers reduce mortality if used for Heart failure

(CBM)

Carvedilol
Bisoprolol
Metroprolol

Which 3 b-blockers prolong survival after MI | TMP

Tiolol Metropolol Propranolol

Which b-blockers help with glaucoma by decrease IOP (intraocular pressure)

Timolol Betaxolol Carteolol **dont use drugs with local anesthetic action On the ey!!

A1 blocker prototype? MOA? Reversible or irreversible?

Prazosin Reversible antagonist of a1 receptors

Effect of a1 blockers?

- prevent vasoconstriction of both arteries + veins - bp reduced by lowering peripheral vasc resistance - relax smooth muscle in prostate - retain Na + H20 if used without a diuretic - improves plasma lipid profiles (increased HDL) or no change

Side effects of a1 blockers

- well tolerated - orthostatic HTN - dizziness - palpitations - headache - less incidence of reflex tachycardia than non-selective a1 blockers because a2 receptor inhibition of NE release from nerve endings is not affected

Clinical uses of b-blockers

Used in men with HTN + benign prostatic hyperplasia

Centrally acting agents are

A2-agonists

A2 agonist prototypes | CM

Clonidine | Methyldopa

MOA of CENTRAL a2 agonists (clonidine + methyldopa)

- Reduce sympathetic flow from vasomotor centers in brainstem - but still allow these centers to retain or increase sensitivity to baroreceptor control - clonidine and methyldopa have slight variation in hemodynamic effects

Clinical use of CENTRAL a2 agonists

Methyldopa = HTN during pregnancy Clonidine = lower bp by decreasing CO, decrease peripheral vasc resistance, and decrease HR + relaxation of capacitance vessels

Side effects of clonidine

Sedation Dry mouth Depression Sexual dysfxn * *transdermal prep has less sedation than oral intake * *abrupt withdrawal = life threatening HTN crisis

Methyldopa effect?

- lowers bp by decreasing PVR, reducing HR + CO | - analog of L-dopa which becomes NE

Side effects of methyldopa

Sedation Dry mouth Lack of concentration Sexual dysfxn