Term
| Which receptor type, in the body, plays a predominant role in bladder emptying? |
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Definition
| M3 Muscarinic cholinergic-3 receptor |
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Term
| Name the three newer uroselective antimuscarinic agents used in OAB and UI |
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Definition
Darifenacin (Enablex),
Oxybutynin (Ditropan),
Tolterodine (Detrol), |
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Term
| What constituent on the structure of the Antimuscarinic (anticholinergic) agents is required for activity and what does it bind to? |
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Definition
| Positively ionized/ionizable nitrogen binds to cholinergic receptors |
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Term
| Where is the site of action in the body for Alpha 1 Receptor Antagonists? And give an example of a prototypic drug in this class |
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Definition
| Peripheral acting, postsynaptic receptor antagonist. Terazosin |
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Term
| What is a chemical structure found commonly in alpha receptor AGONISTS? |
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Definition
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Term
| What is ISA? (Intrinisic sympathomimetic activity) |
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Definition
| When a beta adrenergic receptor ANTAGONIST shows partial AGONIST properties |
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Term
| What is a chemical structure commonly found in many alpha 1 receptor ANTAGONISTS? (Chemical Class) |
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Definition
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Term
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Definition
| Anti-adrenergic; opposing the effects of the sympathetic nervous system |
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Term
| Name a prototypic drug for alpha 1 antagonists that is indicated for both HTN and BPH |
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Definition
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Term
| Quinazoline + Piperazine + Acyl substituents are found in what drug class? |
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Definition
| Alpha 1 receptor ANTAGONISTS |
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Term
| Doxazosin (Cardura XL) is a Alpha 1 Receptor Antagonist that is indicated for ___ but not __ |
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Definition
| Cardura XL is indicated for BPH but not HTN |
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Term
| Where is the site of action in the body for Alpha 2 receptor agonist? And give an example of a prototypic drug in this class |
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Definition
| Centrally acting receptor agonist. Example Clonidine |
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Term
| Where is the site of action in the body for Beta receptor antagonist? And give an example of a prototypic drug in this class |
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Definition
| Peripherally acting beta antagonist. Propranolol |
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Term
| Where is the site of action in the body for mixed Alpha/Beta receptor antagonist? And give an example of a prototypic drug in this class |
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Definition
| Peripheral alpha 1 and nonselective beta receptor antagonist. Carvedilol |
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Term
| What are some side effects of alpha 2 receptor agonists? (Clonidine) |
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Definition
Centrally acting so side effects are CNS related: Drowsiness/Dizziness/Dry mouth
Beneficial in HTN with renal disease
DO NOT discontinue therapy abruptly |
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Term
| What is the chemical structure that is commonly found in Beta receptor antagonists? |
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Definition
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Term
| Give an example of a Non selective Beta Receptor antagonist (w/o) ISA |
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Definition
| Propranolol (Blocks both B1 and B2) Also includes nadolol sotalol and timolol |
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Term
| Give an example of a Nonselective Beta Receptor Antagonist with ISA? |
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Definition
| Pindolol (Blocks both B1 and B2 with partial B agonist)Acebutolol, Cartelol, Penbutolol |
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Term
| Give two examples of a Cardioselective Beta Receptor Antagonist? Which Beta receptor are they selective for? |
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Definition
| Atenolol and Metoprolol are cardioselective for B1 receptors. |
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Term
| What is the chemical structure that is commonly found in Mixed Alpha/Beta receptor antagonists? |
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Definition
| Arloxypropanolamine AND phenylethanolamine. |
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Term
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Definition
| Swapping functional groups present in a chemical compound while maintaining desired biological activity |
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Term
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Definition
| Not a peptide involved in inflammation, pain, vasodilation and capillary permeability |
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Term
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Definition
| A compound administered in an inactive form that is converted to an active form in vivo (inactive --> active) |
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Term
| Transition state analogue |
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Definition
| an enzyme inhibitor that acts by mimicking the transition state of an enzyme catalyzed reaction (ie renin inhibitor) |
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Term
| What is a prototypic drug for Renin inhibitors? |
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Definition
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Term
| What is a prototypic drug for AceI? |
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Definition
| "prils" Enalapril and Lisinopril |
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Term
| What is the MOA/SAR (required structure)for ACEI? |
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Definition
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Term
| What causes the side effects of the ACEI's? |
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Definition
| ACE has multiple biological substrates and contributes to side effects (angioedema, dry hacking cough) Ie. ACEI blocks breakdown of bradykinin to inactive metabolites |
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Term
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Definition
| Endogenous peptide hormone that is one of the most potent vasoconstrictive agents known (there are also ET-2 and ET-3) |
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Term
| IP (prostacyclin/PGI2) receptor |
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Definition
| Subtype of a prostanoid receptor involved with vasodilation. 7Trans membrane G protein coupled receptor (Gs) |
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Term
| ATP sensitive potassium channel |
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Definition
| Type of channel that plays a crucial role in many cellular functions. Target of minoxidil and diazoxide |
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Term
| N-acetyltransferase-2 NAT2 |
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Definition
| Phase II metabolic enzyme known to be polymorphic in humans. Gives rise to fast and slow acetylators |
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Term
| PAH: Pulmonary arterial hypertension |
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Definition
| Disease state involving increased pressure in the pulmonary arteries |
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Term
| Endothelin Receptor Antagonist - What is the MOA and chemical class? Name a Prototypic drug in this theraputic class. |
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Definition
| Blocks binding of endothelin (ET-1) to its receptor on vascular smooth muscle cells. Chemical class - pyrimidines. Prototypic drug - Bosentan |
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Term
| Nitrates: What is the MOA and chemical class? Name a Prototypic drug in this theraputic class. |
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Definition
| NO Donor (increase cGMP levels). Chemical class - Nitrates. Prototypic drug - Nitroglycerin commonly used for angina. Contraindicated with drug PDE5 inhibitors |
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Term
| PDE5 Inhibitor: What is the MOA and chemical class? Name a Prototypic drug in this theraputic class. |
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Definition
| Blocks the activity of PDE5 increasing cGMP levels. Chemical class - pyrazolopyrimidinone. Prototypic drug - Sidenafil. Side effects: Visual and hearing problems. Do not take with nitrates |
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Term
| IP (Prostanoid) Receptor agonist: What is the MOA and chemical class? Name a Prototypic drug in this theraputic class. |
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Definition
| Act as agonists at the IP receptor. Chemical class - prostanoid. Prototypic drug - Epoprostenol |
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Term
| Is every NO containing drug a vasodilator? |
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Definition
| No. Must be attached to a cissile releasable bond |
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Term
| Why are RAAs agents contraindicated in pregnancy? |
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Definition
| IE Micardis and Tekturna RAAS is directly involved in fetal formation |
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Term
| Importance of arylsulfonamide functional group to the activity of carbonic anhydrase inhibitors? |
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Definition
| Arylsulfonamide group on Carbonic anhydrase inhibitors is required for the interaction with the catalytic zinc atom in the active site of carbonic anhydrase (acidic) - ie. acetazolamide |
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Term
| What is the mechanism of action of loop diuretics (high ceiling diuretics)? |
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Definition
| Inhibition of the Na/K/2Cl cotransporter on the ascending loop of henle (ie. furosemide) |
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Term
| What is the MOA and key structural feature of the thiazide diuretic that is important to its SAR? |
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Definition
| MOA: Inhibition of the NA/Cl cotransporter at the distal convoluted tubule. Thiazide markush (electron withdrawing group) required for diuretic activity. R group is primary determinant of diuretic potency and duration of action. Ie. HCTZ or Chlorthalidone |
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Term
| What is an appropriate diuretic agent for use in patients who are hypersensitive to sulfa containing drugs? |
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Definition
| Triamterene (Sodium channel blocker - potassium sparing diuretic) or Ethacrynic acid (1-4 alpha unsaturated ketone) hypokalemia and hypomagnesium becomes a problem |
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Term
| Define mineralcorticoid and give an example |
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Definition
| A hormone that regulates water and electrolyte balance ie. aldosterone |
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Term
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Definition
| Chemical group found in the "tiazem" group of CCBs ie: Diltiazem. Gives negative ionotropic effects |
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Term
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Definition
| "pamil" group of CCBs. Prototypic drug Verapamil. Metabolism by CYP 3A4 gives negative ionotropic effects |
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Term
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Definition
| "pidines" group of the CCB. Prototypic drug: Amlodipine. The dihydropyridine structure is required for activity |
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