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CVS Pharmacology
Cardiovascular system pharmacology-Malik
| Question | Answer |
|---|---|
| What are the uncontrollable factors that increase the risk of hypertension? | 1) Old Age (Especially those over 60) 2) Race (Africans are more likely to develop it as opposed to Hispanics) |
| What are the most recent recommendations of the Joint National Committee for blood pressure patients? *Over 60 | Start medications at blood pressure of ≥150/90mmHg and treat to goal of < 150/90mm Hg |
| What are the most recent recommendations of the Joint National Committee for blood pressure patients? *Under 60 | Start medications at blood pressure of ≥140/90mmHg and treat to goal of ≤ 140/90mm Hg |
| What are the most recent recommendations of the Joint National Committee for blood pressure patients? *Patients with diabetes or kidney disease regardless of age | Start medications at blood pressure of ≥140/90mm Hg and treat to goal of <140/90mm Hg |
| Lifestyle modifications to reduce hypertension risk: | Weight loss (10kg- 5-20 mmHg decrease) DASH diet (8-14 mmHg decrease) Dietary sodium reduction (2-8 mmHg decrease) Physical activity (4-9 mmHg decrease) Moderation of alcohol consumption (2-4 mmHg decrease) |
| What is the DASH diet? | A carbohydrate-low, protein-low diet which mainly focuses on eating fibers |
| What is the function of a2 agonists? | Inhibit the release of noradrenaline , which works on feedback inhibition, reducing the sympathetic outflow |
| Examples of a2 agonists: | Methyldopa (best choice in case of pregnancy) Clonidine (best choice in case of renal failure) |
| Which drugs can deplete adrenaline and noradrenaline? | Guanethidine Reserpine (not used any more) |
| How can we recognize B-blockers? | They all end with the suffix (-lol) |
| Why do we give a1 agonists? | To allow vasodilation to occur |
| Example of a1 agonists: | Prazosin |
| Why do we give hypertensive patients diuretics? | They increase excretion of water and reduce the blood volume |
| Example of diuretics: | Thiazide |
| Function of Angiotensin Converting Enzyme inhibitors (ACE I) | Inhibits the synthesis of Angiotensin II which is the strongest vasoconstrictor in the body |
| What is an example of renin inhibitors? | Aliskiren |
| Action of Ca channel blockers: | Reduce action potential; cause vasodilation |
| Why is increased NO an effective way to reduce hypertension? | It causes vasodilation |
| Potassium channel modulators: | Manipulate the concentration of potassium around the membrane |
| What are the categories of the 11 groups of hypertensive drugs? | 4 sympathetic, 4 kidney related and 3 local mediators |
| Drugs which affect the vasomotor center: | 1) Methyl dopa 2) Clonidine 3) Guanabenz 4) Guanfacine |
| Drugs which affect the sympathetic ganglia: | Trimethaphan |
| Drugs which affect vascular smooth muscle: | 1) Hydralazine 2) Minoxidil 3) Nitroprusside 4) Diazoxide 5) Verapamil (Ca channel blockers in general) 6) Fenoldopam Hunky Muscular Dudes Feel Very Nude |
| Drugs which affect angiotensin receptors of vessels: | Losartan, Valsartan, Candesartan, Eprosartan, irbesartan, telmisartan, and olmesartan |
| Drugs which affect sympathetic nerve terminals | 1) Guanethidine 2) Guandrel 3) Reserpine Rude Guys Get--> on my nerves |
| Main 5 groups of hypertensive drugs: | 1) Diuretics 2) ACEIs 3) B-blockers 4) A1-blockers 5) Ca antagonists |
| When should we use combination therapy for BP patients? | If your patient’s BP is 210/140 |
| Reserpine can be used in combination with which 3 drugs? | 1) a-blocker like prazosine 2) A2 agonist like clonidine 3) Vasodilators like dihydralazine and minoxidil Rudy loves Pretty Cute Ditzy Missies |
| What is the initial first-choice therapy for hypertension according to JNC 6 and 7? | JNC 6: Diuretic or a beta-blocker JNC 7: Thiazide-type diuretics |
| According to JNC 8 what is the treatment for non-black patients? | Thiazide, ACEI, ARB, or CCB |
| According to JNC 8 what is the treatment for black patients? | Thiazide or CCB |
| For all patients with Chronic Kidney Disease (CKD); initial (or add-on) therapy for hypertension should include | ACEI or ARB (for black and non-black patients) |
| 3 groups of diuretics are used in the treatment of hypertension: | 1- Thiazide diuretics : most commonly used 2- Potassium sparing diuretics 3- Loop diuretics |
| Mechanism of action of Thiazide diuretics: | Decrease the blood pressure by depleting the body's Na stores -inhibition of Na+ reabsorption in the distal tubules of the kidneys . First 4 weeks of administration- patient's blood pressure will decrease by decreasing blood volume |
| In the 4 weeks after administration of diuretics, the patient will experience: | Frequent urination |
| The highest efficacy in reduction of blood pressure by thiazide drugs is about | 15 mmHg |
| This efficacy is considered: | Low, so thiazides are used with other drugs |
| Postural hypotension is rarely observed except: | In the elderly |
| The main site of action of thiazide diuretics is | on the distal tubules |
| What percentage of the reabsorption of Na is inhibited? | 3-5% |
| The main drug of choice of the treatment of hypertension with signs of edema | Loop diuretics |
| Loop diuretics are associated with | Hypovolemia and electrolyte imbalance ( hypocalcemia ,hypomagnesemia , hypokalemia ) |
| The most important prototypes of thiazide diuretics are: | 1- Chlorothiazide : given orally 1-2 times a day 2- Hydrochlorothiazide : 1-2 times a day |
| Thiazide is usually administered under low dose of | 12.5-25 mg (or up to 50mg in extremes ) |
| Low doses of thiazide exert as much antihypertensive effect: | As higher doses |
| Side effects appear at which dosage of thiazides? | Over 50mg |
| What are the side effects of thiazides? | 1) Hypokalemia 2) Hyperglycemia : due to inhibition of K+ dependent insulin release 3) Hyperlipidemia : rise in total LDL level which increases the risk for strokes 4) Hyperuricemia due to drug-drug interaction between thiazide and uric acid |
| Inhibited excretion of uric acid causes it to accumulate in the body, resulting in gout. This side effect is really prominent in patients taking thiazide over: | A long time (about 10 years) even under low doses |
| The prototype drug of loop diuretics is | Furosemide commonly known as Lasix |
| Lasix must be dosed at least | Twice daily |
| Lasix must be administered during the day or at lunch to avoid | Nocturia |
| Adverse effect of loop diuretics is summarized in: | 1) Ototoxicity especially with aminoglycosides 2) Hyperurecemia and hypocalcemia |
| ACE inhibitors are: | The best drugs in the treatment of hypertension regarding the patients situation |
| ACEI drugs end with the suffix | -pril |
| The main prototype drug of ACEIs is: | Captopril |
| ACE inhibitors inhibit the enzymatic activity of angiotensin converting enzyme found in the lungs and this is going to produce the following actions : | 1- Reduce the amount of angiotensin 2 by inhibiting the conversion of angiotensin 1 to angiotensin 2 2- Prevent the conversion of bradykinin to an inactive metabolite by ACE which is going to increase the amounts of bradykinin in the body |
| Angiotensin 2 has two important functions : | 1) Potent vasoconstrictor 2) Stimulates the production of aldosterone from the adrenal cortex which stimulates the reabsorption of Na+ and water from kidney tubules |
| Inhibition of Angiotensin 2 causes: | 1- Vasodilatation of vessels 2- Diuretic action by inhibiting the reabsorption of Na+ and water by kidney tubules |
| Side effects of ACEIs: | 1) Dry cough in 10% of patients 2) Angioedema 3) Hyperkalemia 4) First-dose syncope |
| In those patients who develop dry cough we switch them into | ARBs |
| Angioedema complications: | Excessive vasodilatation and increased vascular permeability Rapid accumulation of fluid in the neck Fluid accumulation in the neck creates a huge risk for airway obstruction and suffocation which is a medical emergency |
| The only case when the hyperkalemia becomes significant is | When we use spironolactone along with ACEI because spironolactone is an aldosterone antagonist |
| Therapeutic uses of ACEIs | 1) Congestive heart failure in order to reduce the levels of angiotensin 2 which further damage the heart 2) Treatment of hypertension in patients with diabetes or chronic renal disease 3) Diabetic nephropathy |
| Why are ACEIs used in CHF? | Angiotensin 2 increases myocardial force of contraction Patients with congestive heart failure have increased level of angiotensin 2 because of hypovolemia caused from the low pumping action of the heart |
| Why are ACEIs used in treatment of hypertension in patients with diabetes or chronic renal disease: | Vasoconstriction of renal arterioles which rises intra glomerulus pressure and reduces glomerular filtration rate is caused by angiotensin 2 |
| Angiotensin 2 receptor antagonists are used: | as an alternative to ACEI and are mainly used if the patient can't tolerate the side effects of ACEI |
| Angiotensin 2 receptor blockers (ARB ) are drugs that end with the suffix | -sartan |
| ARB main prototype is: | Losartan |
| ARB have the same efficacy as ACEI and they have the same: | Therapeutic uses and the same side effects EXCEPT dry cough and Angioedema because they don't increase bradykinin levels |
| ARB and ACEI are | Teratogenic drugs Category X, never give to pregnant women |
| Alternative pathways of angiotensin 2 production other than ACE: | 1- Chymase enzyme which converts angiotensin 1 to angiotensin 2 2- Nonrenin protease cathepsin t-PA which converts angiotensinogen to angiotensin 2 directly |
| Why do we use ARB drugs in this case? | This alternative pathway can sometime overcome the inhibition of angiotensin 2 production by ACEI |
| In the case of ACEI and ARB, we only combine these two drugs because: | We really don't want any angiotensin 2 to be produced at all |
| ACEIs are contraindicated in: | 1) Pregnancy 2) Bilateral renal artery stenosis |
| Which drugs are recommended agents when the preferred first-line agents are contraindicated: | Calcium channel blockers |
| Action of calcium: | Calcium enters muscle cells through special channels and produce contractility in them |
| Mechanism of action of CCBs: | CCBs block L-type channels and stop the inward movement of Ca into the cell They exert their hypotensive effect through their vasodilation effect on the vessels It will cause a negative inotropic and chronotropic activity on the heart |
| Chemical Classes of CCBs: | 1- Diphenylalkylamines 2- Benzothiazepines 3- Dihydropyridines |
| Diphenylalkylamines are represented by: | Verapamil |
| Action of Diphenylalkylamines | Have no selectivity towards Ca channels wherever in the body; they block those in vessels and in the heart. They result in hypotension ( vasodilation effect) They produce both negative inotropic and chronotropic effect |
| Benzothiazepines represented by | Diltiazem |
| Action of Benzothiazepines: | Have less selectivity towards the heart that ranges between the 1st and 3rd classes and more selective within the vessels |
| Dihydropyridines represented by: | Nifedipine Amlidopine |
| Action of Dihydropyridines: | Selective within vessels and have no effect on heart channels |
| Coronary artery dilation is induced by which of these 3 drugs? | All of them Can be used in Angina Pectoris |
| Peripheral artery dilation is induced by which of these 3 drugs? | Nifedipine The greatest effect on the vessels and in cases of isolated HTN it’s the drug to be used |
| Which drugs cause negative inotropic effect? | Nifedipine has only little effect on it unlike Varapamil and Diltiazem |
| Slowing AV conduction is done by which drug? | Varapamil Decrease heart rate in addition to its negative inotropic effect. Contraindicated in bradychardic patient |
| Drug which causes greatest increase in cardiac output? | Nifedipine Decreases peripheral resistance against the heart pumping Decreases the afterload and allows for greater cardiac output |
| Heart rate will increase at very low concentrations of nifedipine. This problem has been overcome by: | 1) Designing a sustained release formula called a "one dose daily". Sustained release nifedipine is better than the regular 3-times-a-day nifedipine and avoids the peak and trough transition 2) A drug with a longer half-life |
| Which drug is used to overcome the problems? | NORVASC A form of Amlodipine that has a very long half-life and produces little fluctuation in plasma drug concentration due to its sustained release formula and can be used in angina. These drugs are also one dose daily drugs |
| Uses of CCBs: | 1) Verapamil and Diltiazem are used in arrhythmias because they have an effect on the heart 2) If a patient doesn’t have arrhythmias but has HTN use Nifedipine 3) Nifedipines can be combined with B-blockers |
| NWhich situations can we not use certain drugs in? | In congestive heart failure, Verapamil and Diltiazem are contraindicated Contraindicated in drug with negative inotropic/chronotropic effects with them- we might end up with 2nd/3rd stage AV block Can’t combine them with beta blockers that affect SA AV |
| The most prominent side effects associated with CCBs are: | 1- Headaches 2- Ankle swelling/edema 3- Constipation 4- Gingival hyperplasia |
| CCBs do not affect concentrations of | plasma cholesterol or triglycerides or extracellular calcium hemostasis |
| Beta-adrenergic Blockers end with the suffix: | -lol |
| B blockers can be which types? | 1) Selective 2) Non selective and vasodilating 3) Non selective |
| Selective target: | Beta 1 rather than 2 |
| Non selective and vasodilating target: | Beta 1, beta 2, and alpha 1 |
| Non selective target: | Beta 1 and 2 |
| Examples of selective B-blockers: | Metoprolol Acebutolol Atenolol Esmolol Aristocrats Eat Alligator Meat |
| Examples of non-selective and vasodilating B-blockers: | Labetolol Carvedilol |
| Examples of non-selective B-blockers: | Propanolol Penbutolol Pindolol Timolol Nadolol Sotalol |
| These drugs were previously used in the 4-drug regimen used to treat HTN. Why did they stop? | Low efficacy |
| Their efficacy is at most | 10 mmHg |
| Uses of B-blockers: | Angina pectoris Atrial fibrillation Cardiac arrhythmia CHF Essential tremor Glaucoma Hypertension Migraine prophylaxis: to reduce the stress Mitral valve prolapse Pheochromocytoma with α-blocker Symptomatic control in anxiety & hyperthyroidism |
| Propranolol is : | Non-selective (B1 and B2) Reduces cardiac output and renin release. BlockingB2however is not desirable because it causes bronchospasm Lipophilic, meaning it can cross blood brain barrier easily Drug of choice for prophylaxis against migraines |
| Atenolol& Metoprolol are: | Cardioselective drugs Most widely used blockers in treatment of HTN (affect rennin release) and have no carbohydrate effect |
| Pindolol & acebutolol & penbutolol are : | Partial agonists some sympathomimetic activity. They lower blood pressure by decreasing resistance and appear to depress cardiac output less than other blockers Use in patients with bradyarrythmias or peripheral vascular disease |
| Labetalol and carvidalol are: | Totally nonselective; alpha 1, beta 1 and beta 2 blockers They cause vasodilation by blocking the alpha 1 receptors Useful in the management in pheochromocytoma and hypertensive emergencies Peripheral vascular disease |
| Characteristics of Esmolol: | Rapid onset of action Short half-life 9-10 minutes (through constant I.V infusion). Good drug of choice In management of intra and postoperative hypertension Hypertensive emergencies when associated with tachycardia Vasodilators and muscle dilators |
| Why shouldn't you stop B-blockers suddenly? | Sudden withdrawal may cause rebound hypertension |
| Why may it cause rebound hypertension? | When we give beta-blockers for a long time, our bodies respond by upregulating the number of beta receptors so they become more sensitive toward adrenaline |
| Examples of selective a1 blockers: | 1) Alfuzosin 2) Doxazosin 3) Prazosin 4) Terazosin Alpha Dogs Tread Proudly |
| Functions of a1 blockers: | Alpha 1 receptors cause vasoconstriction Alpha 1 blockade causes vasodilation and reduces blood pressure |
| Are a1 blockers good drugs for hypertension? | No |
| Then, why are they used? | For management of hypertension in patients with prostatic hyperplasia Because they block alpha receptors on the prostate Naïve hypertensive patients, as well |
| Main side effects of a1 blockers: | Hypotension First dose syncope |
| How is first dose syncope avoided? | Start the drug with one-third the dose instead of the full dose |
| If the patient has prostatic hyperplasia but does not have hypertension then you use: | alpha blockers selective for alpha 1-A which is only found on the prostate and not on blood vessels |
| Example of drug that only blocks alpha1-A and are used for normotensive patients with prostatic hyperplasia is: | Silodosin |
| Examples of Alpha 2 receptor agonist: | 1) Clonidine 2) Methyldopa |
| Function of a2 agonists: | alpha 2 receptors cause feedback inhibition on the sympathetic system and noradrenalin release Alpha 2 agonists reduce sympathetic activity and decrease blood pressure |
| Clonidine is used to treat: | Mild to moderate hypertension that has not responded adequately to treatment with diuretics alone |
| Why is Clonidine used to treat hypertension complicated with renal disease? | Does not reduce renal blood flow, unlike ACEIs |
| Therefore in the cases of bilateral renal artery stenosis, we use: | 1) Clonidine 2) CCBs |
| Difference between action of methyldopa and Clonidine: | Clonidine lowers heart rate and cardiac output more than methyldopa |
| Withdrawal of clonidine after protracted use, particularly with high dosages (more than 1 mg/d), can result in: | Life- threatening hypertensive crisis mediated by increased sympathetic nervous activity |
| After omitting one or two doses of the drug, patients exhibit which symptoms? | Nervousness, Tachycardia Headache Sweating |
| If the patient stops the drug suddenly, this will over-activate α1 & α2. Which drug do we use to block these receptors? | Labetalol |
| The most important thing you need to know about methydopa is: | It is the drug of choice used in pregnant women with hypertension |
| Why is it used in pregnant women? | It does not reduce cardiac output and perfusion to the baby |
| Methyldopa especially valuable in treating hypertension with | Renal insufficiency |
| Before giving methyldopa to pregnant hypertensive women, we give: | MgCl2 |
| The most common side effect of methyldopa is: | Sedation |
| Side effects of clonidine and methyldopa include: | Dry mouth and nasal mucosa Sedation Hallucination Depression |
| What are some examples of vasodilators? | 1) Fenoldopam 2) Nitroprusside 3) Hydralazine 4) Diazoxide 5) Minoxidil |
| What is the functions of these vasodilators? | Smooth muscle relaxants Reflex stimulation of the heart resulting in increasing the myocardial contractibility, heart rate, and oxygen consumption Increase plasma renin concentration |
| Reflex stimulation of the heart can cause which unwanted effects? | Prompt angina and myocardial Infarction in predisposed individuals |
| Increased plasma renin concentration causes: | sodium and water retention |
| These unwanted effects can be blocked by | combination with a diuretic and a beta blocker |
| How does Nitroprusside work? | By release of nitric oxide |
| Nitroprusside is the drug of choice in which situation? | Hypertensive emergency |
| Why is it the drug of choice? | Because it has activity on BOTH veins and arteries, unlike vasodilators(only arterial) |
| If there is kidney injury, what should we use instead? And why? | Fenoldopam, because Nitroprusside reduces kidney perfusion |
| What is Fenoldapam? | D1 receptor agonist |
| Function of Hydralazine | Smooth muscle relaxant Produces reflex stimulation of the heart Mainly by releasing NO and EDRF |
| When is Hydralazine used? | To treat moderately severe hypertension, in combination with diuretics and beta-blockers |
| Hydralazine monotherapy is accepted method of controlling blood pressure in | Pregnancy induced hypertension AFTER methyldopa |
| Side effects of Hydralazine: | Arrhythmia Precipitation of angina Lupus-like syndrome can occur with high doses, but is reversible |
| What is a hypertensive emergency? | A rare but life threatening condition Normal person: DBP is > 150 mm Hg with SBP > 210 Individuals with preexisting conditions: DBP of > 130 mm Hg |
| What are some examples of pre existing complications? | Encephalopathy Cerebral hemorrhage Left ventricular failure Aortic stenosis |
| If BP is not reduced rapidly, what will occur? | hypoperfusion of vital organs would be compromised |
| Drugs used for treatment of hypertensive emergency | 1) Sodium nitropresside (onset 1-2 min), is the drug of choice is administered IV 2) Labetalol (a and b blocker), (onset 5-10 min) given IV bolus or infusion 3) Fenoldopam (onset 2-5 min), D1 receptor agonist also given as an IV infusion |
| Major limitation of Labetolol: | Long half-life(3-6 hr) that prevents rapid titration |
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Ulaisl
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