Antihypertensives Ii

Front 1

Clonidine

Back 1

Catapress, also methyldopa

Front 2

Pharmacologic class of Clonidine

Back 2

central alpha-2 agonist

Front 3

Therapeutic class of Clonidine

Back 3

antihypertensive

adjunct to Rx of opiod withdrawal, prophylaxis of migraine

Front 4

Pharmacodynamics of Clonidine

Back 4

stimulates alpha-2 adrenoreceptors in brainstem, thereby leading to downregulation of sympathetic output

Front 5

Pharmacokinetics of Clonidine

Back 5

onset is 1 hour
duration is 8 hours
F = 85%

also available as a cutaneous patch

Front 6

Toxicity of Clonidine

Back 6

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

Front 7

Interactions of Clonidine with other drugs

Back 7

additive effects with most other antihypertensives; additive sedation with other CNS drugs

Front 8

special considerations with Clonidine

Back 8

pregnancy class C

avoid in patients with renal insufficiency

Front 9

Indications and dose/route of Clonidine

Back 9

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

Front 10

Monitoring Clonidine

Back 10

follow BP and HR

Front 11

Trimethaphan

Back 11

Arfonad

Front 12

Pharmacologic class of Trimethaphan

Back 12

GANGLIONIC BLOCER

Front 13

Therapeutic class of Trimethaphan

Back 13

antihypertensive

Front 14

Pharmacodynamics of Trimethaphan

Back 14

blocks nicotinic transmission with both sympathetic and parasympathetic ganglia

produces veno- and vaso- dilatation

Front 15

Pharmacokinetics of Trimethaphan

Back 15

useful only when give IV

produces fall in BP within minutes; partly metabolized and partly excreted by kidneys

Front 16

Toxicity of Trimethaphan

Back 16

watch out for sudden, severe drop in BP, also fall in HR

also reduction in just about any sympathetic or parasympathetic response

Front 17

Interactions of Trimethaphan with other drugs

Back 17

additive effects with most other antihypertensives

NSAIDS may reduce ability to lower BP

hyperkalemia with KCL, others

Front 18

Special considerations of Trimethaphan

Back 18

patients are quite miserable

hence only used during general anesthesia

also, helpts to tilt patient to help control BP

Front 19

Indication and dose/route for Trimethaphan

Back 19

given by IV infusion and only to treat HTN crisis or for controlled hypotension during surgery

Front 20

Monitoring with Trimethaphan

Back 20

minute to minute monitoring of BP (and HR)

Front 21

Pharmacologic class of Reserpine

Back 21

Rauwolfia alkaloid

Front 22

Therapeutic class of Reserpine

Back 22

antihypertensive

Front 23

Pharmacodynamics of Reserpine

Back 23

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

Front 24

Pharmacokinetics of Reserpine

Back 24

good oral bioavailability, but biological effects take 2-3 weeks to develop

Front 25

Toxicity of Reserpine

Back 25

dizziness, orthostatic hypotension, depression

Front 26

Interactions of Reserpine with other drugs

Back 26

additive effects with most other antihypertensives

Front 27

Special considerations of Reserpine

Back 27

approved by FDA in 1953

first antihypertensive drug approved and first sympatholytic drug approved by the FDA

Front 28

Indications and dose/route of Reserpine

Back 28

for HTN, 0.1 - 0.2 mg po q day

Front 29

Monitoring of Reserpine

Back 29

BP, sympathetic tone, depression!!!!

Front 30

Atenolol

Back 30

Tenormin

also propranolol and metaprolol

Front 31

Pharmacologic class of Atenolol

Back 31

beta adrenoceptor blocker

(beta-1 specific)

Front 32

Therapeutic class of Atenolol

Back 32

antihypertensive, antiarrhythmic, primary and secondary prevention of MI, anti-anginal

Front 33

Pharmacodynamics of Atenolol

Back 33

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)

Front 34

Pharmacokinetics of Atenolol

Back 34

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)

Front 35

Toxicity of Atenolol

Back 35

excessive hypotension, bradycardia

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

worsen bronchospasm in severe asthmatics

Front 36

Interactions of Atenolol with other drugs

Back 36

additive effects with most other antihypertensives, additive AV block with CEBs

Front 37

Special considerations for Atenolol

Back 37

may be especially useful in HTN patients with exertional angina, MI, atrial fibrillation

WATCH OUT FOR ABRUPT WITHDRAWAL

Front 38

Indications and dose/route for Atenolol

Back 38

for treatment of hypertension, 25-100mg per day, in one or two doses

Front 39

Monitoring of Atenolol

Back 39

BP and HR

Front 40

Prazosin

Back 40

Minipress

also Terazosin

Front 41

Pharmacologic class of Prazosin

Back 41

alpha 1 adrenoreceptor blocker

Front 42

Therapeutic class of Prazosin

Back 42

antihypertensive, treatment of BPH, treatment of Raynaud's syndrome

Front 43

Pharmacodynamics of Prazosin

Back 43

blocks alpha-1 receptors on arterioles and veins, thereby inhibiting NE-mediated vasoconstriction and venoconstriction

Front 44

Pharmacokinetics of Prazosin

Back 44

available po or transdermal

variable oral bioavailability (~60%)

onset is 2 hours

duration is 12-24 hours

EXTENSIVELY METABOLIZED IN LIVER

Front 45

Toxicity of Prazosin

Back 45

excessive hypotension with passing out, especially orthostatic, especially in patients on diuretics

Front 46

Interactions of Prazosin with other drugs

Back 46

additive effects with most other drugs, especially diuretics

Front 47

Special considerations with Prazosin

Back 47

start gradually, and at bedtime, to avoid first-time passing out

Front 48

Indications and dose/route of Prazosin

Back 48

as monotherapy, begin with 1mg tid, advance to 20 mg per day divided tid

Front 49

Monitoring with Prazosin

Back 49

BP, weight, and edema

Front 50

Labetalol

Back 50

Normodyne, Trandate

Front 51

Pharm class of Labetolol

Back 51

alpha and beta receptor blocker

Front 52

Therapeutic class of Labetalol

Back 52

antihypertensive

Front 53

Pharmacodynamics of Labetolol

Back 53

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

Front 54

Pharmacokinetics of Labetalol

Back 54

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

Front 55

Toxicity of Labetalol

Back 55

avoid in patient with bradycardia, heartblock, CHF, asthma, shock

use with caution in patients with cardiomyopathy, pheochromocytoma

Pregnancy class D

Front 56

Interactions with other drugs and Labetalol

Back 56

additive effects with most other antihypertensives

Front 57

Special considerations of Labetalol

Back 57

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)

Front 58

Indications and dose/route for Labetalol

Back 58

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

Front 59

Monitor for Labetalol

Back 59

BP and HR