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59 Cards in this Set

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Clonidine
Catapress, also methyldopa
Pharmacologic class of Clonidine
central alpha-2 agonist
Therapeutic class of Clonidine
antihypertensive

adjunct to Rx of opiod withdrawal, prophylaxis of migraine
Pharmacodynamics of Clonidine
stimulates alpha-2 adrenoreceptors in brainstem, thereby leading to downregulation of sympathetic output
Pharmacokinetics of Clonidine
onset is 1 hour
duration is 8 hours
F = 85%

also available as a cutaneous patch
Toxicity of Clonidine
withdraw gradually; risk of bradycardia in sinus node disease

lethargy, fatigue, depression, ALLERGY TO SULFA ANTIBIOTICS

cause K and Mg depletion

cause Na and Cl depletion, metabolic alkalosis, volume depletion; worsen hyperuricemia
Interactions of Clonidine with other drugs
additive effects with most other antihypertensives; additive sedation with other CNS drugs
special considerations with Clonidine
pregnancy class C

avoid in patients with renal insufficiency
Indications and dose/route of Clonidine
being with 0.1 mg po bid, up to 1.2 mg per day

transdermal begin with 0.1mg per 24 hours as a 7-day patch
Monitoring Clonidine
follow BP and HR
Trimethaphan
Arfonad
Pharmacologic class of Trimethaphan
GANGLIONIC BLOCER
Therapeutic class of Trimethaphan
antihypertensive
Pharmacodynamics of Trimethaphan
blocks nicotinic transmission with both sympathetic and parasympathetic ganglia

produces veno- and vaso- dilatation
Pharmacokinetics of Trimethaphan
useful only when give IV

produces fall in BP within minutes; partly metabolized and partly excreted by kidneys
Toxicity of Trimethaphan
watch out for sudden, severe drop in BP, also fall in HR

also reduction in just about any sympathetic or parasympathetic response
Interactions of Trimethaphan with other drugs
additive effects with most other antihypertensives

NSAIDS may reduce ability to lower BP

hyperkalemia with KCL, others
Special considerations of Trimethaphan
patients are quite miserable

hence only used during general anesthesia

also, helpts to tilt patient to help control BP
Indication and dose/route for Trimethaphan
given by IV infusion and only to treat HTN crisis or for controlled hypotension during surgery
Monitoring with Trimethaphan
minute to minute monitoring of BP (and HR)
Pharmacologic class of Reserpine
Rauwolfia alkaloid
Therapeutic class of Reserpine
antihypertensive
Pharmacodynamics of Reserpine
binds to vesicles that contain NE or serotonin, preventing their uptake, and ultimately depleting the neuron of NE (or serotonin)

this effect takes 2-3 weeks to develop, and including neurons, and also the adrenal medulla
Pharmacokinetics of Reserpine
good oral bioavailability, but biological effects take 2-3 weeks to develop
Toxicity of Reserpine
dizziness, orthostatic hypotension, depression
Interactions of Reserpine with other drugs
additive effects with most other antihypertensives
Special considerations of Reserpine
approved by FDA in 1953

first antihypertensive drug approved and first sympatholytic drug approved by the FDA
Indications and dose/route of Reserpine
for HTN, 0.1 - 0.2 mg po q day
Monitoring of Reserpine
BP, sympathetic tone, depression!!!!
Atenolol
Tenormin

also propranolol and metaprolol
Pharmacologic class of Atenolol
beta adrenoceptor blocker

(beta-1 specific)
Therapeutic class of Atenolol
antihypertensive, antiarrhythmic, primary and secondary prevention of MI, anti-anginal
Pharmacodynamics of Atenolol
binds directly to beta-receptors, with a preference for beta-1 over beta-2, leading to lower blood pressure via several potential mechanisms (less cardiac output, less activation of the RAA system)
Pharmacokinetics of Atenolol
available po or iv, variable oral F

onset 1-2 hours

duration 12-24 hours

can be given once per day

RENALLY EXCRETED (longer half life)
Toxicity of Atenolol
excessive hypotension, bradycardia

heart block can worsen severe CHF (but indicated for mild to moderate CHF)

worsen bronchospasm in severe asthmatics
Interactions of Atenolol with other drugs
additive effects with most other antihypertensives, additive AV block with CEBs
Special considerations for Atenolol
may be especially useful in HTN patients with exertional angina, MI, atrial fibrillation

WATCH OUT FOR ABRUPT WITHDRAWAL
Indications and dose/route for Atenolol
for treatment of hypertension, 25-100mg per day, in one or two doses
Monitoring of Atenolol
BP and HR
Prazosin
Minipress

also Terazosin
Pharmacologic class of Prazosin
alpha 1 adrenoreceptor blocker
Therapeutic class of Prazosin
antihypertensive, treatment of BPH, treatment of Raynaud's syndrome
Pharmacodynamics of Prazosin
blocks alpha-1 receptors on arterioles and veins, thereby inhibiting NE-mediated vasoconstriction and venoconstriction
Pharmacokinetics of Prazosin
available po or transdermal

variable oral bioavailability (~60%)

onset is 2 hours

duration is 12-24 hours

EXTENSIVELY METABOLIZED IN LIVER
Toxicity of Prazosin
excessive hypotension with passing out, especially orthostatic, especially in patients on diuretics
Interactions of Prazosin with other drugs
additive effects with most other drugs, especially diuretics
Special considerations with Prazosin
start gradually, and at bedtime, to avoid first-time passing out
Indications and dose/route of Prazosin
as monotherapy, begin with 1mg tid, advance to 20 mg per day divided tid
Monitoring with Prazosin
BP, weight, and edema
Labetalol
Normodyne, Trandate
Pharm class of Labetolol
alpha and beta receptor blocker
Therapeutic class of Labetalol
antihypertensive
Pharmacodynamics of Labetolol
reduces BP by blocking access of NE to beta-receptors and alpha-1 receptors, thereby lowering BP by several different mechanisms, patients differ in degree of beta-blockade vs. alpha-blockade
Pharmacokinetics of Labetalol
excellent absorption but high first pass effect

leading to F-25%

onset 1-2 hours po

2-5 minutes when given IV

Extensively metabolized in liver by IID6
Toxicity of Labetalol
avoid in patient with bradycardia, heartblock, CHF, asthma, shock

use with caution in patients with cardiomyopathy, pheochromocytoma

Pregnancy class D
Interactions with other drugs and Labetalol
additive effects with most other antihypertensives
Special considerations of Labetalol
use reduced doses in patients with impaired liver function

dizziness is most troubling early side effect

most often used for hypertensive crisis (as with nitroprusside)
Indications and dose/route for Labetalol
most commonly given iv with initial small boluses of 20mg, followed by continuous infusion at 2 mg/min

not usually give po for chronic treatment...80 mg thrice daily, or 240 mg SR once daily
Monitor for Labetalol
BP and HR