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89 Cards in this Set
- Front
- Back
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Angiotensin converting enzyme inhibitors
ACEi |
captopril (Capoten)
enalapril (Vasotec) lisinopril (Prinivil, Zestril) quinapril (Accupril) ramipril (Altace) benazepril (Lotensin) etc… |
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ACEi
MOA |
Highly selective drugs that inhibit the conversion of Ang. I (Inactive) to Ang II (Active) which interferes with aldosterone & renin release
All have similar therapeutic indications (CHF and Hypertension), ADR, and contraindications |
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ACEi
Effects |
Reduce angiotensin II and aldosterone levels = Reduced vasoconstriction
Systemic arteriolar dilation & increase compliance of larger arteries which lowers systemic vascular resistance and (mean, diastolic and systolic) BP |
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ACEi
Clinical applications |
Hypertension
Heart failure, diabetes |
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ACEi
Uses in HTN |
Monotherapy in mild-moderate (50%).
Combo with BB, CCB, or diuretics (90%) |
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ACEi
Side Effects HAD NAB |
Hypotension (High Plasma Renin Activity and CHF)
Angioedema Dry cough due to increase bradykinin levels (5-20%) Not during pregnancy Acute renal failure Bilateral renal artery (or solitary) stenosis (can lead to acute renal failure) |
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ACEi
DDI |
Hyperkalemia:
Especially if used in conjunction with K+ sparing, K+ supplements, NSAIDS, Beta Blockers |
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Angiotensin II-receptor antagonists
ARBs |
losartan
candesartan irbesartan valsartan, etc… |
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ARBs
MOA |
Competitive binding but often insurmountable antagonism.
Slow dissociation ARB-induced receptor internalization Allosteric antagonism |
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ARBs
Effects |
Same as ACEi but with no increase in bradykinin
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ARBs
Clinical applications |
Hypertension
Heart failure |
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ARBs
Uses in HTN |
All ARBs are approved for hypertension treatment (Combination with hydrochlorothiazide)
A number of studies suggest that ARBs are just as good as ACE inhibitors (No cough and less incidence of angiodema than ACE inh.) |
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ARBs
Side Effects |
Not given during pregnancy (teratogenic potential)
Careful in Renal Stenosis |
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ARBs
DDI |
Hyperkalemia
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Diuretics
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Thiazides
chlorthalidone hydrochlorothiazide metolazone, etc… |
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Why use thiazides for HTN?
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Thiazides and related diuretics are the most frequently used class of antihypertensive agents in the US
Antihypertensive effects when used alone (monotherapy) occurs with small doses Enhance antihypertensive effects of virtually all other drugs and can be used to prevent/reverse the salt and water retention caused by other antihypertensive drugs |
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Thiazides
MOA |
Block of NCC1 (Na/Cl transporter) in DCT & prevents Na+ from being reabsorbed.
Water stays with Na+, so diuresis occurs. |
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Thiazides
Effects |
Reduce blood volume plus poorly understood vascular effects
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Thiazides
Clinical applications |
Hypertension
Mild heart failure |
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Thiazides
Side effects/ADR |
Hypokalemia (Urinary K+ Loss)- Fatal arrhythimias
Erectile Dysfunction Gout due to hyperuricemia (rare) Hydrochlorothiazide rapid hyponatremia Hypercalcemia Changes in plasma lipids (increase LDL) and glucose intolerance |
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Thiazides DDI
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NSAIDS: Inhibit synthesis of prostaglandin synthesis and decrease antihypertensive effect
Quinidine- Torsade de Points Digitalis toxicity- arrhythmias Corticosteroids- Amplify the hypokalemia effects Li+- Decrease clearance and increase toxicity |
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Loop Diuretics MOA
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Block of NKCC2 in Loop of Henle & prevents Na+ from being reabsorbed. Water stays with Na+, so diuresis occurs.
Decrease in electrical potential, therefore lose Na+, Ca++, and K+ Less effective for BP & possibly detrimental |
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Loop Diuretics
Effects |
Like thiazides except with greater efficacy
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Loop Diuretics
Clinical applications |
Severe hypertension
Heart Failure |
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Loop Diuretics
Side effects/ADR |
Toxicity:
Hypokalemic metabolic alkalosis Ototoxicity (dose related) Hyperuricemia (can trigger gout) Hypomagnesemia Allergic reactions (for ones that are sulfonamides) Dehydration Contraindications: Allergy to sulfonamides |
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Loop Diuretics DDI
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Co administration with aminoglycosides may increase ototoxicity
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Aldosterone Receptor Antagonists
(K+ Sparing) MOA |
Reduce kaliuresis and potentiate the hypotensive effects
Mechanism can be inhibited by NSAIDs due to their inhibition of renal prostaglandin production |
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Aldosterone Receptor Antagonists
Effects |
Increase Na & decrease K excretion
Poorly understood reduction in heart failure mortality |
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Aldosterone Receptor Antagonists
Clinical applications |
Hypertension
Heart failure Aldosteronism |
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Aldosterone Receptor Antagonists
(K+ Sparing) Side effects/ADR |
Hyperkalemia
Hyperchloremic metabolic acidosis Gynecomastia (with spironolactone but not eplerenone) Acute renal failure (combine triamterene with indomethacin) Kidney stones (triamterene) Dosage adjustment for triamterene and spironolactone in liver disease |
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Aldosterone Receptor Antagonists
(K+ Sparing) DDI |
Combined use of CYP3A4 inhibitors and eplerenone
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Renin Inhibitors
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aliskiren
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Renin inhibitor
MOA |
Inhibits enzyme activity of renin
It binds with high affinity to plasma renin Reduces PRA & concentrations of AngI, AngII and aldosterone |
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Renin inhibitor
Effects |
Reduces angiotensin I and II and aldosterone
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Renin inhibitor
Clinical applications |
Hypertension
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Renin inhibitor
Side effects |
Skin rash, diarrhea, headache, cough, hypotension, & angioedema
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Renin inhibitor
DDI |
Diuretics and ARB (synergism effect)
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Sympatholytics
Alpha-1 Antagonists |
Prazosin
Terazosin Doxazosin |
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Sympatholytics
Alpha-1 Antagonists MOA |
Selectively block alpha-1 adrenoreceptors
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Sympatholytics
Alpha-1 Antagonists Effects |
Prevent sympathetic cardiac stimulation
Reduce renin secretion |
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Sympatholytics
Alpha-1 Antagonists Clinical applications |
Hypertension
BPH (benign prostatic hyperplasia) |
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Sympatholytics
Alpha-1 Antagonists Side effects/ADR |
1st Dose Effect
Reflex tachycardia Arrhythmias Orthostatic Hypotension & Syncope (30-90 min) Blurred vision Headache and dizziness Sexual dysfunction |
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Sympatholytics
Alpha-1 Antagonists DDI |
Any drug that can affect BP
PDE-5 inhibitor (e.g., sildenafil) Changes in the free fraction- Drugs that compete for the plasma protein α1-acid glycoprotein (e.g. Olanzapine, Fluoxetine) |
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Sympatholytics
α1 & 2 receptors irreversible antagonist |
Phenoxybenzamine (Dibenzyline)
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Sympatholytics
α1 & 2 receptors irreversible antagonist MOA |
Decrease Peripheral Resistance
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Sympatholytics
α1 & 2 receptors irreversible antagonist Uses |
Short-Term Control of Hypertension
Pheochromocytoma Hypertensive Crisis (MAO inhibitors) Clonidine withdrawal |
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Sympatholytics
α1 & 2 receptors irreversible antagonist Side effects/ADR |
Induce reflex cardiac stimulation
Tachycardia, arrhythimias, & ischemia Enhance Norepinephrine Secretion GI stimulation |
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Sympatholytics
α1 & 2 receptors irreversible antagonist DDI |
Tadalafil (theoretical)
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Sympatholytics
Selective α2 Receptor Agonist |
Clonidine (Duraclon®)
Guanfacine (Wytensin) Guanabenz (Tenex) |
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Sympatholytics
Selective α2 Receptor Agonist MOA |
Activate alpha-2 adrenoreceptors
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Sympatholytics
Selective α2 Receptor Agonist Effects |
Suppressing Sympathetic Output in the CNS (Brainstem)
Increasing Vagal Tone Inhibiting Release of Norepinephrine and Ach (GI) |
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Sympatholytics
Selective α2 Receptor Agonist Clinical applications |
Hypertension
Clonidine is also used in withdrawal from abused drugs |
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Sympatholytics
Selective α2 Receptor Agonist ADR |
Clonidine ADR-
CNS side effects: Nightmares, restlessness, & depression Dry Mouth and Sedation (50% of pts) Postural Hypotension & Marked Bradycardia Sexual Dysfunction Hypertensive Crisis (withdrawal) |
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Sympatholytics
Selective α2 Receptor Agonist DDI |
Clonidine DDI-
Pts taking other drugs that suppress AV conduction. BBB+CCB = Bradycardia & Sinus arrest Diuretics and other anti-hypertension agents |
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Sympatholytics
Beta Blockers Non-selective b1/b2 1st Generation |
Nadolol (Corgard)
Propranolol (Inderal) Pindolol [ISA] (Visken) Penbutolol [ISA] (Levatol) TImolol (Blocadren) |
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Sympatholytics
Beta Blockers Selective b1 (cardioselective) 2nd Generation |
Acebutolol (Sectral)
Atenolol (Tenormin) Bisoprolol (Zebeta) Esmolol (hospital setting) Metoprolol (cardioselective at lower doses b1 heart and kidneys..loses selectivity with increase in dose) |
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Sympatholytics
Beta Blockers Selective b1 3rd Generation |
Betaxolol
Celiprolol Nebivolol |
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Sympatholytics
Beta Blockers Non-subtype 3rd Generation |
Carvidolol (b1,b2,a1, antioxidant)
Coreg used for HTN,CHF, patients with left ventricular dysfunction post MI Carteolol (Cartrol) Bucindolol (b1,a1,b2 agonist) Labetolol (Trandate, Normodyne) (b1,b2,a1,ISA b2) use for HTN during pregnancy |
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Sympatholytics
Beta Blockers MOA |
Blockade of β1-Receptors of the Juxtaglomerular Complex
Reduce renin secretion & production of Ang. II Other BB may decrease CO or decrease peripheral vascular resistance to various degrees depending on cardioselectivity |
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Sympatholytics
Beta Blockers Effects |
Reduction in:
Myocardial contractility Heart Rate Cardiac Output CNS sympathetic output Firing of peripheral adrenergic neurons |
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Sympatholytics
Beta Blockers Clinical Applications |
Mild to moderate HTN
Useful in preventing reflex tachycardia in SEVERE HTN from other HTN meds Reduce mortality in post MI and HF patients |
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Sympatholytics
Beta Blockers ADR/SE |
Careful in pts with:
1. Reactive airway disease (asthma) 2. Sinoatrial or atrioventricular nodal dysfunction 3. Patients with bradycardia 4. Patients with insulin-dependent diabetes BB without ISA increase concentration of triglycerides and lower HDL Sudden discontinuation lead to rebound hypertension Tissue sensitivity to endogenous catecholamines -Epinephrine: hypertension & bradycardia |
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Sympatholytics
Beta Blockers DDI |
Not used in combination with drugs that:
Inhibit AV conduction (verapamil) Nonsteroidal antiinflammatory drugs (e.g. indomethacin) Additive antihypertensive effects in conjunction with Diuretics Administration of Epinephrine can produce severe hypertension and bradycardia..alpha 1 are not being blocked will get innervated |
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Beta Blocker
Sympatholytic Effects |
Blocking a1,b1,b2
a1: lowers HR, SV, TPR b1: heart increases HR and contractile force and rate of relaxation b2-pulmonary: bronchial smooth muscle contraction b2-brain: decrease sympathetic flow b2-vasculature: cause dilation |
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Calcium Channel Blockers
Dihydropyridines & Clinical Applications |
Amlodipine (Norvasc)
Nifedipine (Adalat, Procardia) Felodipine (Plendil) Hypertension |
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Calcium Channel Blockers
Non-dihydropyridines & Clinical Applications |
Verapamil (Calan, Isoptin)
Diltiazem (Cardizem) Hypertension, angina, arrhythmias |
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CCC: Dihydropyrines
MOA & Effects |
Block vascular calcium channels more so than cardiac calcium channels
Reduce arterial vascular tone (afterload) |
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CCC: Non-dihydropyridines
MOA & Effects |
Non-dihydropyridines:
Prevent calcium influx into myocytes AND smooth muscle lining arteries and arterioles by blocking L-type calcium channels Reduce arterial vascular tone (afterload) Reduce HR + contractility → reduce O2 requirement Verapamil & Diltiazem have direct negative chronotropic effects. |
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Inhibition of transmembrane movement of Ca++ through voltage sensitive Ca++ channels.
1. Effects on the vasculature 2. Effects on the Heart (non-dihyropyridines) 3. Uses |
CCB lower BP by relaxing ARTERIOLAR smooth muscle and decreasing peripheral vascular resistance
Effects on the Heart: Have no effect on the AV node but Non-dihyropyrines effect Ca-channels in the heart Mild to moderate hypertension in the elderly & African Americans |
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CCC
ADR/Side effects |
Ankle edema, headache, flushing, palpitation
Headache, dizziness and flushing Peripheral Edema Increased hydrostatic pressure in lower extremities due to precapillary dilation and reflex postcapillary constriction Aggravate gastroesophageal reflux Inhibition of smooth muscle contraction of the esophageal sphincter Constipation (common for verapamil) Bradycardia & sinoatrial node arrest (verapamil & diltiazem) |
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CCC
DDI |
Verapamil blocks the P-glycoprotein drug transport. Thus it will affect any drug that is eliminated by this mechanism
Increase plasma concentration of Digoxin CCB and Quinidine (Na+, K+, α, M2) can cause excessive hypotension Verapamil or Diltiazem and β-blockers |
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Vasodilators
Never 1st line |
Diazoxide
Hydralazine (Apresoline) Methyldopa (Aldomet) Minoxidil Nitroprusside |
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Vasodilators
Minoxidil MOA |
Opens K+ channels in vascular smooth muscle
Not 1st choice; 3rd or later |
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Vasodilators
Minoxidil Effects |
K + efflux and Hyperpolarization, cant depolarize & not much vasoconstriction..only works on arterial side
Increase blood flow to skin, skeletal muscle, the GI and heart more than to the CNS It enhances venous return to the heart and SNS output, which leads to an increase in CO It only works in the ARTERIOLES NOT VEINS |
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Vasodilators
Minoxidil Clinical Applications |
Efficacious in pts with the most severe and drug resistant forms of hypertension
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Vasodilators
Minoxidil ADR/Side effects |
1. Fluid and Salt Retention
2. Increased proximal renal tubular reabsorption 3. Reduced renal perfusion and stimulation of α adrenergic receptor 4. Can be given with a loop diuretic Cardiovascular 1. Baroreceptor-mediated activation of SNS 2. Increase HR, myocardial contractility, and myocardial O2 consumption 3. Can be given with a β-blocker Hypertrichosis- Growth of hair in the face, back, arms, and legs |
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Vasodilators
Hydralazine MOA & Effects |
Direct relaxation of arteriolar smooth muscle via nitric oxide release. Doesn't effect veins
Reduces vascular resistance |
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Vasodilators
Hydralazine Clinical Applications |
Severe Hypertension or hypertensive emergencies (e.g. preeclampsia)
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Vasodilators
Hydralazine ADR/Side effects |
Headache, Nausea, flushing, Hypotension, palpitations, reflex tachycardia, dizziness, Salt Retention and ANGINA PECTORIS.
Not given to pts with coronary artery disease Combine with a β-blocker and a diuretic |
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Vasodilators
Hydralzaine DDI |
Drug induced lupus syndrome and other autoimmune reactions (e.g. serum sickness, vasculitis, glomerulonephritis, etc…)
Dose dependent, Acetylator Phenotype, and Race |
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Vasodilators
Nitroprusside MOA & Effects |
Powerful nitrovasodilator that acts by releasing nitric oxide (NO)
Mimic the production of NO by vascular endothelial cells Increase in intracellular cGMP Dilates both arterioles and venules (non-selective) Modest increase in HR Overall reduction in myocardial demand for oxygen |
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Vasodilators
Nitroprusside Clinical Applications |
Hypertensive emergencies
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Vasodilators
Nitroprusside ADR/Side effects |
Due to excessive vasodilation
Conversion of nitroprusside to cyanide and thiocyanate Given with sodium thiosulfate |
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Vasodilators
Diazoxide MOA & Effects |
Vasodilates arteriolar smooth muscle vessels by activating K+ channels (Hyperpolarization)
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Vasodilators
Diazoxide Clinical Applications |
IV only for the treatment of severe hypertension (rarely used)
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Vasodilators
Diazoxide ADR/Side effects |
Salt and water retention
Tachycardia and myocardial ischemia Hyperglycemia (inhibit the excretion of insulin from pancreatic β cells) Hypertrichosis (excessive hair growth includes the face) |
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Vasodilators
Methyldopa MOA & Effects |
Prodrug (analog of dopa)
Stimulates CENTRAL (acting) alpha adrenoreceptors by alpha-methylnorepinephrine or alpa-methyldopamine Reduces vascular resistance by decreasing sympathetic tone |
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Vasodilators
Methyldopa Clinical Applications |
Hypertension during pregnancy
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Vasodilators
Methyldopa ADR/Side Effects |
CNS effects
Sedation, depression, reduction in libido, Parkinsonian signs and hyperprolactinemia Dry mouth ADR’s unrelated to its pharmacology 1. Hepatotoxicity (rare but serious SE) 2. Hemolytic anemia (20%) 3. Autoantibodies directed at the Rh antigen on erythrocytes 4. Treat with glucocorticoids to alleviate symptoms |
