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21 Cards in this Set
- Front
- Back
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How do kidneys control BP
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Baroreceptors in kidneys
Decrease in arterial BP---> Kidneys secrete Renin (secreted when Na low)--> Renin coverts Angiotensinogen to Angiotension I----> Angiotension II in lungs by ACE |
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Most potent vasoconstrictor in the body
Constricts arteries and veins, INCREASING BP Increases GFR Stimulates Aldosterone secretion which increases Na reabsorption--> increase in blood volume--> increase BP |
Angiotension II
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1. Heart Failure: Increase renin secretion by juxtaglomerular cells in response to low renal perfusion
Increase renin secretion in response to sympathetic stimulation due to decrease perfusion Renin increases Angiotension II Aldosterone Increases---> NaCl and H2O reabsorption---> increase blood volume High levels angiotension II BAD on heart causing remodeling and fibrosis |
Antagonists of Renin-Angiotension System
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Drug of choice for Heart Failure
Inhibit conversion Angiotension II, Decrease vasoconstrictive effects on arterioles and veins, inhibit metabolism of bradykinin (increasing dilating effect) Effect: Vasodilation Aldosterone secretion is decreased, decrease Na and H2O retention, decreasing blood volume and BP |
ACE Inhibitors
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1. Sulfhydryl Group (Captopril)
2. Dicarboxyl Groups 3. Phosphorous Groups (Fosinopril) |
Three groups ACE Inhibitors
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ACE Inhibitors are ester pro-drugs and differ from one another in 3 ways
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1. Potency
2. Whether the pharmacological effect is due to the parent compound or it's metabolite 3. Pharmacokinetics (extent of absorption, with or without food, T1/2, distribution, and route of excretion) Differ in TISSUE DISTRIBUTION |
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All block Angiotension I from becoming Angiotension II
1. Therapeutic indications 2. Adverse effects 3. CI |
ACE Inhibitors Similarities
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What ACE Inhibitors are not excreted by the kidneys
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Fosinopril and Spirapril (excreted by liver and kidneys)
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Which pts should the dose of ACE Inhibitors be reduced?
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Impaired renal function b/c increase duration of plasma conc---T1/2
Pts with elevated plasma renin activity; they have a hyper-reactive response (pts with HF and Na depletion)---induced hypotension |
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Pro-drug of epinephrine
Increases the lipid solubility by 600x vs epinephrine Ocular penetration is 16X that of epinephrine Biochemically altered to improve kinetics but does not participate in pharm effect |
Dipivefrin---Propine
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1. Propine
2. Prostaglandins (Latanoprost, Travaprost, Bimatoprost, Tafluprost) 3. Valacyclovir---> Acyclovir 4. Famciclovir---> Penciclovir 5. Bacampicillin--> Ampicillin 6. L-Dopa--> Dopamine 7. Nevanac--> Amfenac |
PRO-DRUGS
Amoxicillin is not the pro-drug of Ampicillin Acyclovir = pre-drug |
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Bioavailability 75%
Peak plasma conc in 1 HR T1/2: 2 HRS 40-50% excreted unchanged Food decreases bioavailability by 25-30%, dose 1hr BEFORE meals Dose 6.25mg - 150mg bid to tid |
ACE INHIBITORS with Sulfydryl groups
Captopril |
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Pro-drug, cleaved in liver to Benazeprilat--dicarboxylic acid form
More potent than capyopril, lisinopril, enalapril Rapidly 37% absorbed Completely metabolized Peak plasma conc: 1/2-1 hr for benazepril, 1-2 hr for benazeprilat T1/2 10-11 hrs ONLY ACCUMULATES IN THE LUNG Dose: 5-80mg/day |
ACE INHIBITORS with Dicarboxylic groups
Benazepril (Lotensin) |
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Enalapril maleate is the pro-drug of the carboxylic acid enalaprilat
60% absorbed NOT DECREASED BY FOOD Peak levels in 1hr; Peak of enalaprilat 3-4hrs T1/2 1.3hrs for enalapril; 11hrs for enalaprilat Dose: 2.5mg-40mg HF 2.5mg; HTN 5mg |
ACE INHIBITORS with Dicarboxylic groups
Enalapril (Vasotec) |
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Primarily for IV
HTN: 0.625-1.25mg IV over 5 min, repeat every 6 hrs as needed |
ACE INHIBITORS with Dicarboxylic groups
Enalaprilat |
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Lysine analog of enalaprilat, ACTIVE
Slowly 30% absorbed Peak conc in 7 hrs T1/2: 12 hrs Excreted unchanged in kidneys Dose 5mg-40mg HF 5mg; HTN 10mg |
ACE INHIBITORS with Dicarboxylic groups
Lisinopril---NOT A PRO DRUG |
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Pro drug converted to moexiprilat
Bioavailability 13%, GREATLY REDUCED BY FOOD Take 1 hr before meals Peak conc. 1.5hrs T1/2 2-12hrs Dose 7.5mg-30mg If on diuretics or renal impairment dosage should be reduced 50% |
ACE INHIBITORS with Dicarboxylic groups
Moexipril (Univasc) |
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Perindopril erbumine is a pro-drug metabolized to the active form perindopirlat
Bioavailability 75% not affected by food Peak 3-7hrs Exhibits BIPHASIC elimination T1/2 3-10hrs as major component of elimination and 30-120hrs as it dissociates from tissue ACE Dose 2-16mg |
ACE INHIBITORS with Dicarboxylic groups
Perindopril (Aceon) |
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Pro-drug hydrolyzed to quinaprilat
Bioavailability 60%, may be reduced by food Excreted in urine and feces Peaks 2hrs BIPHASIC Dose 5mg-80mg Conversion to quinaprilat is reduced if liver damage |
ACE INHIBITORS with Dicarboxylic groups
Quinapril (Accupril) |
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Pro-drug converted to ramiprilat
Bioavailability 50-60% RATE not extent of absorption affected by food Peaks 3hrs TRIPHASIC ELIMINATION Dose 1.25mg-20mg |
ACE INHIBITORS with Dicarboxylic groups
Ramipril (Altace) |
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Pro-drug converted to trandolaprilat (8X more potent)
Bioavailability 70% Excreted in urine and feces Peaks 4-10hrs BIPHASIC Plasma clearance decreased by renal insufficiency and diminished hepatic function Dose 1mg-8mg |
ACE INHIBITORS with Dicarboxylic groups
Trandolapril (Mavik) |
