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Pharm > Block 2-Reymann (AntiHypertensive) > Flashcards

Block 2-Reymann (AntiHypertensive) Flashcards

1
Q

Classes of drugs

A
  • 5 classes:
  1. Diuretics
  2. Beta-Adrenoreceptors ANTAgonists
  3. Ca-channel blockers
  4. Inhibitors of Angiotensin
  5. Alpha adrenergic blockers (?)
  • Hypertension is NOT an isolated disease &linked w:
  • increased coronary artery
  • MI
  • Left vent hypertrophy
  • Also Stroke & peripheral vascular disease
  • All lead to CV remodeling in LV dysfunction
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2
Q

Resperine (obsolete)

A
  • _PK: _
  • Oral with 1/2 life of 24 hours & can presist up to 6 weeks
  • PD:
  • Depletes biogenic amines from neuronal vesicles <u><strong>(ALL NT)</strong></u> by inhibiting re-uptake
  • SE:
  • Denervation of **SNS & PSNS **
  • Nasal congestion
  • Hypersecretion <u><strong>(BAD FOR ULCERS)</strong></u>
  • Bronchoconstriction
  • mental Depression
  • Parkinsons
  • SUICIDE
  • Use:
  • Not used due to long term presistance (6weeks)
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3
Q

Clonodine (alpha-2) PK&PD

A
  • Alters sympathetic activity-GI coupled-LESS NE = Lowered<strong> B1 effect</strong>
  • Alpha-2 autoreceptor sympathomimetic <u><strong>(mimcs)</strong></u> 2nd choice in hypertension treament
  • PK:
  • **Oral, IV, & Patch **
  • !/2 life of 8-12 hours secreted renally
  • PD:
  • Centrally mediated hypotensive effects
  • Reduces CO - Reduce sympathetic tone, relax of venous, reduction of peripheral resistance
  • Renal blood flow maintained = Initial hypertensive episode<u><strong> (renin-angiotensin)</strong></u>
  • CNS effects
  • Body adapts w/rebound effects <u><strong>(Lowered TPR &amp; HR)</strong></u>
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4
Q

Clonodine (alpha-2) Use&SE

A
  • SE:
  • Seen in high doses due to <strong>blockage of SNS</strong>
  • BradyCardia
  • AV block
  • Functional cardiac failure (left vent activity)
  • Dry mouth
  • Drowsiness
  • Constipation
  • Tricyclic Anti-depress lower effects of Anti-hyper effects
  • Use:
  • 2nd line for hypertension
  • Treat withdrawl symptoms heroin, alcohol,benzos <strong>(OPIATES)</strong>
  • prevention of alcoholic delirium
  • adjunct w/analog-sedation need less of other drug <u><strong>(DEXMEDETOMIDINE)</strong></u>
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5
Q

Methyldopa (alpha-2)

A
  • Alters SNS w/GI coupled = LESS NE lowered Beta-1
  • Centrally acting (<strong>act on brain from sending signals</strong>) anti-hypertensive SAFE in pregers
  • PK:
  • Oral 1/2 4-6 hours
  • up to 24 hours MOA
  • PD:
  • Centrally mediated hypotensive effects similar to clonodine (<u><strong>alpha 2 autoreceptor</strong></u>)
  • SE:
  • same as clonodine
  • Coombs test MAY turn + for pregers
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6
Q

Prazosin, Terazosin, Doxazosin (A1 blockers)

A
  • PK:
  • Oral & IV
  • 1/2 life 3-4 hours (prazosin)
  • OR 22hours (doxazosin)
  • PD:
  • Blocks alpha-1 receptors = Dialate vessels
  • reflex tachycardia (B1 still works) due to lowered Arterial & venous resistance
  • NO effect on Pre-synap a-2 autoreceptor
  • Decrease tone on urinary sphinctors = Treat BPH
  • SE:
  • First dose phenomenon-Sensitive when given drug frist time = Orthostatic hypertension <u>LEAD TO MI</u>
  • Dizziness & palpatations
  • Test + for ANA
  • Good effect on Lipid profile
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7
Q

Hypertension & Diuretics

A
  • Thiazide used for hypertension Even in small doses
    Use K+ supplements or combine w/K+sparring dieuretics WATCH Hyperkalemia
  • Keeping pt on dry weight may further help bypertension COULD lead to dehydration:
  • Mental confusion
  • Aggravate COPD
  • Peripheral arterial occulsive disease
  • SE:
  • Hypokalemia
  • Hyperuricaemia
  • Imparied glucose tolerance
  • Hyperlipidemia (chornic usage)
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8
Q

Beta Blockers

A
  • Non-selective: Propranalol
  • Contraindicated in pregers due to B2 in uterus = dialation premature delivery
  • Contraindicated in Diabetes = hypoglycemic episodes going unseen
  • Small doeses of B-blockers good for CHF
  • Beta 1 (little effect on B2): Atenolol & metoprolol
  • Alpha & Beta 1 blocker: Labetalol <u><strong>(intensive care)</strong></u> 4 isomers
  • Beta 2 agonist-lower BP BUT does NOT constrict peripheral vessels
  • Alpha & Beta 1 blocker: Carvedilol (not perscribed as often)-USED in remote cases for <u><strong>lipid profile</strong></u>
  • Beta 1 agonist: Esmolol <u><strong>(short acting) </strong></u>emergency cases
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9
Q

Comparing Beta to Alpha (Anti-hypertensive)

A
  • _A-blockers: _
  • Better @ managing lipid profile <u><strong>(person w/high cholesterol)</strong></u>
  • A-1 blockers do NOT affect insulin sensitivity & will NOT cause cold extermity syndrome
  • B-blockers:
  • tend to increase LDL & decrease HDL = Increase TAGs
  • Do NOT cause orthostatic hypotension or reflex tachycardia
  • OVERALL beta-blockers are the dug of choice
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10
Q

CCB (Ca+2 channel blockers) PK&PD

A
  • Drugs: Verapamil, Dilitiazam, Nifedipine
  • Given to pt with contraindications for B-blockers<u><strong> (ASTHMATIC, DIABETICS, PREGERS)</strong></u>
  • PK:
  • Oral & IV
  • Highly bound to serum proteins
  • Hepatic metab & renal excretion
  • PD:
  • Blocks L-type Ca+2 channels <u><strong>(work on phase2 plateu)</strong></u>-Verapamil
  • Cardiodepressant - Vasodialator <u>(dilitiazam)</u>
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11
Q

CCB (Ca+2 Channel blockers) SE & use

A
  • SE:
  • **Dihydropyridines (Nifedipines)- **
  • EXCESSIVE vasodilation = reflex tachycardia
  • Tachycardia = Dizziness, headache, flushing, digital dysaethesia (numb), Edema, constipation
  • Verapmil & Dilitiazem-
  • Cardio depressents = Bradycardia due to NO reflex <u><strong>(Antiarrthymthmic</strong></u>)
  • USE:
  • All used to treat hypertension
  • Treat Arrythmia <strong>(Verapmil & Dilitiazem)</strong>
  • Treat Angina with ALL 3 depends on what outcome u want <u><strong>(bradycardia or NOT)</strong></u>
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12
Q

CCB & Beta

A
  • Chronic use of CCB can result in increased risk of MI due to rebound effects-
  • Aburptly STOP or forget dosage
  • Can be treated with longer 1/2 lives OR gradual onset
  • Amlodipine<u><strong><em><strong> </strong></em>(dihydropyridine)</strong></u> long acting w/SLOW onset
  • Beta & CCB routinely used in combo in treating hypertension-
  • Combining the 2 = LESS of each drug leading to LESS effect of substance LOAD on BODY
  • Amlodipine(vasodialation) decrease in contractile force <u><strong>WHICH</strong></u> can lead to reflex Tachycardia
  • Block reflex w/B-Blocker =OVERadditive Effect <u><strong>(override bodies natural mech)</strong></u>
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13
Q

Inhibitors of Angiotensin

A
  • Can be used instead of CCB/B-blockers
  • Include ACE-inhibitors & AT1-blockers
  • AT-1 blockers Creates a perfusion shunt = Activation of Angio 2
  • Vasocontriction
  • Aldosterone secretion
  • NE release
  • Prodrugs=Lostratan/Valsar_tan _
  • ACE inibitiors:
  • Vasodialation-Decrease aldesterone-Decrease NE release
  • BradyKinin is INACTIVE by Kinase 2 (ACE)
  • Bradykinin = Vasodialation (Prostacyclin, NE, edothelial factors)-Inflammation
  • Prototype Drug=Captopril, Enalapril, lisinopril
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14
Q

ACE-Inhib (Captopril) PK & PD

A
  • PK:
  • Oral & Renal elimination
  • PD:
  • Angiotensin 2 Antagonism (blocks)
  • Decreased vasoconstriction-NE decrease-Decrease in aldosterone
  • Brady kinin=Vasodialation
  • NE decrease=
  • NO reflex tachy or CO change
  • NO water & sodium retention
  • Reduction in SNS tone
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15
Q

ACE-Inhib (Captopril) SE&CI

A
  • SE:
  • Hypotension
  • Dry cough & bronchospasm due to ++ of bradykinin
  • Skin Rashes
  • Angioneuroticedema<u><strong>(HIVES)</strong></u>, neutropenia <u><strong>(LOW NEUTROPHILS)</strong></u>, leukipenia<u><strong>(DECREASED WBC)</strong></u> DUE to inflammation via prostaglandins & bradykinin system
  • Taste perversion
  • Hyperkalemia (inhibition of aldesterone)
  • Protenuria
  • CI:
  • Pts w/HIstory of renal artery stenosis & renal filaure
  • Angioedema, Asthma, COPD
  • Pregers cause oligohyrdaminion <u><strong>(def of)</strong></u>
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16
Q

ACE-Inhib (Captopril) Interactions

A
  • Drug interactions:
  • NSAIDS block bradykinin pathway=reduce anti-hypertensive <u><strong>(vasodialtion)</strong></u>
  • K+ sparing diuretics = accelerated HYPERkalemia
  • Increased LVLs of Digoxin & Lithium
  • Toxicity:
  • Hypotension w/o tachy due to NE depression
  • Therapeutic Drug combo:
  • ACE inhib + K+wasting diuretic (low doses)
  • K+ wasting diuretics = increased ACE system effect
  • Over-additive antihypertensive effect
17
Q

ACE-inhib (Enalapril/Enalaprilat)

A
  • Prodrug=Enalapril
  • PK:
  • Oral 1/2 life of 11hrs
  • Renal elimination
  • Enalaprilat given IV in hypertensive Emergency
  • PD:similar to captopril
  • SE:
  • More potent w/<u><strong>SLOWER </strong></u>onset & <u><strong>LONGER </strong></u>duration
  • NO SULFA groups
  • NO taste pervertion
  • Fosinopril & Moexipril = HEPATIC elimination
18
Q

Use of ACE inhibitors

A
  • ACE-Treatment of:
  • Hypertension
  • CHF
  • Post MI (due to dead cells around the infarction generate Arrythmias)
  • B-Blockers preferred POST MI but for Pts with contraindication <u><strong>(asthma/Diabetics) </strong></u>ACE inhibit given
  • Progressive renal disease=Diabetic neuropathy
  • AT-1 & AT-2 Blockers Treat:
  • AT-1-
  • normally mediate vasocontriction, NE, aldosterone
  • Helps w/Vascular & cardiac remodeling(<u><strong>chronic CHF/Hypertension)</strong></u>
  • AT2-_ANTI-prolif effect _
19
Q

Angtiotensin 2/AT-1 Blocker (Losartan)

A
  • Direct acting
  • PK:
  • Oral
  • 1/2 life 2hrs active metabolite 6-9hrs
  • Hepatic elimination
  • PD:
  • Like ACE inhib BUT no effect on bradykinin
  • Decreased vastocontriction, decreased NE release, Decreased aldosterone
  • _SE: _
  • LIke ACE NO bradykinin related issues (<u><strong>NO angioedema &amp; NO dry cough)</strong></u>
  • CI:
  • Renal artery stenosis = Renal failure
  • Pregers
20
Q

Contraindication (COPD & Asthma)

A
  • NO B-blockers (propanonlol)
  • NO Ace-inhibitors (Enalapril)
  • Reason:
  • Induction of broncospams
  • Dry cough
  • USE AT-1 blockers (Losartan), CCB, or Alpha Blockers
21
Q

Contraindication (bradycardia)

A
  • NO clonidine (beta)
  • B-blockers
  • Verapamil (CCB)
  • Dilitiazem (CCB)
  • Reason:
  • Aggrevation & risk of Adam’s Stokes Syndrome (passing out due to heart arrthymia)
22
Q

Contraindication (Diabetes & gout)

A
  • DM:
  • NO thiazides
  • NO unselective B-blockers (colonopin)
  • Reason:
  • Reduce glucose tolerance
  • Reduce symptoms of Hypoglycemia
  • Gout:
  • NO Thiazides
  • Reason:
  • Reduction of uric acid secretion=GOUTY attack
23
Q

Contraindication (Coronary & peripheral artery disease)

A
  • CAD:
  • NO Hydralazine (vasodialator)
  • NO Prazosin (Alpha-1 blocker)
  • Reason:
  • Triggered Angina-pectoris VIA reflex tachy
  • PAOD:
  • NO beta blockers
  • Reason:
  • Triggered periphery artery occulsion disease

Pharm (14 decks)

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