Pharm Cardio List Flashcards
Atropine
Mechanism
Non-selective muscarinic blocker. Decrease HR, Contraction, and AV Node
Atropine Contraindicated
With use of Viagra (NO produces GMP and Viagra blocks its breakdown
Epinephrine
On Target Effects
Selectivity
Vasoconstrictor locally, increases HR, CO through B
ALL
Norepinephrine
On Target Effects
Selectivity
Increase BP through A
a1, a2, b1
Dobutamine
On Target Effects
Selectivity
Increase HR and CO
B1
Phenylephrine
On Target Effects
Selectivity
Increase BP through A
a1
Ephedrine
Mainly increase BP through A, but HR/ CO thorugh B
Centrally-acting alpha-2a agonists
Clonidine Methyldopa (pro)
Centrally-acting alpha-2a agonists
Mechanism
Agonist of postsynaptic A2a in Rostral Ventrolateral Medulla
Centrally-acting alpha-2a agonists
On Target Effects
Decreases sympathetic outflow of CO and/or Vascular Resistance by stimulating CNS receptors Major Compensatory responses is Na Retention Decrease Insulin Secretion
Methyldopa (pro)
Unusual Facts
Use in pregnancy
Positive Coombe’s Test
Treat HTN in preclampsia
Sedation
Reserpine
Mechanism
Prevents Dopamine Transfer to Vesicle through VMAT by destroying adrenergic synaptic receptor
Reserpine
On Target Effects
Depletes NE; reduces TPR, CO, and BP. Major Compensatory response is Na Retention
Reserpine
Side Effects
Depression, sedation, dry mouth,
night terrors
Alpha-Blockers
Mechanism
Reduce Vascular Resistance and Venous Return. Block Glucose Production. Not as good for essesntial HTN
Phenoxybenzamine
Mechanism
Binds to A receptor covalently; irreversible and non-competitive
Phenoxybenzamine
Indication
Selectivity
Side Effect
Pheocromocytoma
A1, A2
Raynaud’s phenomenon
Prazosin
Selectivity
Side Effect
A1 Orthostatic HTN (Prazosin), Syncope
Alpha-Blockers
Name
Phenoxybenzamine
Phentolamine
Prazosin
Phentolamine
Prazosin
Mechanism
Block receptors on arterioles and venules. Competitive antagonists.
(Decrease Phase 4)
Beta-Blockers
Mechanism
Block Beta Receptor, decreases sympathetic outflow,
Beta-Blockers
On Target Effects
Reduce CO, then start to reduce Vascular Resistance as well. Reduce Renin release from the kidney. Block Glucose production. Decrease Insulin secretion. Activate HSL; lowers HDL and increases TG’s Angina
Propanolol (MS)
Also blocks?
Bind and block fast Na channels responsible for rapid depolarzation of fast response cardiac AP’s
Labetalol
Also blocks?
Also blocks A1
Nebivolol
Special
Indication
Antioxidant; NO production
Metabolic Syndrome HTN
Betaxolol
Special
Selectivity
Ca entry blockade
B1
Beta-Blockers
Contraindicated
Asthmatics, COPDl, and HF patients and Diabetics (NS ones)
Direct Vasodilators (Selective arteriolar smooth muscle relaxer)
Nitroprusside (prodrug)
Minoxidil (Rogaine)
Nitroprusside (prodrug)
Mechanism
Release of NO from drug or endothelium
Nitroprusside (prodrug)
On Target Effects
Indication
Side Effect
Forms NO; Causes relaxation. Dilates both arteries and veins
Drug of choice for malignant HTN &
HTN emergency
Hypotension, palpitations, tachycardia, cyanide
Minoxidil (Rogaine)
Mechanism
Open K channels, causing hyperpolarization of vascular smooth muscle
Minoxidil (Rogaine)
On Target Effects
Side Effect
Relaxes arterial smooth muscles.
Hirsutism
Powerful activatator of Renin
(compensatory)
L-Type Calcium Channel Blockers
Name
Phenylalkylamine (Verapamil)
Benzothiazepine (Diltiazem)
L-Type Calcium Channel Blockers
Mechanism
Block L-type Calcium channels in Cardiac and Smooth Muscle
Phenylalkylamine (Verapamil)
On Target Effects
Selectivity
Rapid cycle; Require open channel; Decrease HR
Myocardium
Benzothiazepine (Diltiazem)
On Target Effects
Slow cycle; Require certain Voltage; Decrease HR
L-Type Calcium Channel Blockers
Contraindicated
Side Effect
Beta Blockers: Synergistic with SA Node Digoxin
Constipation, edema, headache, bradycardia, GI problems, dizziness, AV block, tachycardia
Dihydropyridines
Name
Amlodipine
Nifedipine
Nicardipine
Nimodipine
Amlodipine
Mechanism
On Target Effects
Block L-type Calcium channels in Cardiac and Smooth Muscle.
Decreases BP by relaxing arteriolar smooth muscle. Very mild changes
Angina
Dihydropyridines
Side Effects
Edema, Reflex sympathetic response, Hypotension, Constipation
Gingival Hyperplasia
ACE Inhibitors
Name
Captopril
Lisinopril
Enalapril (prodrug)
Ramipril
ACE Inhibitors
Mechanism
On Target Effects
Blocks formation of Angiotensin II, decreasing Aldosterone
Lower TPR and BP, dilates vessels
ACE Inhibitors
Indication
Contraindicated
Side Effects
Diabetes, Heart Failure, CKD, Stroke
Renal Disease Pregnancy
Cough, hyperkalemia, Hypotension,
AR Blockers
Losartan (prodrug)
Candesartan
AR Blockers
Mechanism
On Target Effects
Block Angiotensin II at AT receptor, decreasing aldosterone.
Vasodilation, high Na secretion, low TPR, CO, and BP.
AR Blockers
Contraindicated
Renal Disease Pregnancy
Renin Inhibitors
Aliskerin
Aliskerin
Mechanism
On Target Effects
Side Effects
Inhibits Renin
Decrease Ang I and therefore Ang II and Aldosterone
Hyperkalemia
Nitrates
Name
Nitroglycerin
Nitroglycerin Mechanism On Target Effects Indication Contraindicated Side Effects
NO activates cGMP Venodilates (lowers Preload and afterload), coronary vasodilation Angina Give with Beta Blockers Sildenafil (Viagra) (type V PDE) Hypotension, Headache, Racs
ANTIARRHYTHMIC DRUGS
Classes
Class I (Na Blockers) Class II (Beta Adrenoceptor Blockers) Class III (K Blockers) Class IV (Ca Blockers) Digitalis Glycosides (Vagotonic) Adenosine Receptor Agonist
Class I (Na Blockers) Drugs
Procaineamide
Lidocaine
Flecanide
Procaineamide Mechanism On Target Effects Notes Indication Side Effects
Suppresses ectopic pacemaker activity in partially depolarized cells slows conduction even at slow rates.
Prolongs AP (block K as well); slows conduction even at slow rates. > 1
Class I don’t effect SA Node
A or V Fib Torsades (3)
Drug induced LUPUS Torsades de Pointes
Lidocaine On Target Effects Indication Contraindicated Side Effects
Rapid dissociation; will fall off by normal HR. Slows conduction of fast HR Least likely to have negative effects Ventricular Tachycardia Torsades (2) NOT atrial or prophylactic
Flecanide
Mechanism
On Target Effects
Contraindicated
Suppress automaticity, increases RefractoryDissociation is very slow
Organic or structural heart disease
Class II (Beta Adrenoceptor Blockers) MP
Propranolol
Metoprolol
Propranolol
Selectivity
B1, B2
Metoprolol
Selectivity
B1
Metoprolol
On Target Effects
Slow SA Node (agent of choice)
Class III (K Blockers)
Class III (K Blockers)
Amiodarone
Sotolol
Ibutilide
Class III (K Blockers) Mechanism On Target Effects
Increase refractory period by prolonging repolarization
Prolongs phase 3, prolonging the ERP. Shows prolongation of QT Interval
Amiodarone
Indication
Side Effects
A/V arrhythmias Torsades (1)
Pulmonary Fibrosis, Hyperthyroidism, Hepatitis
Sotolol
Notes
Contraindicated
Side Effects
Beta blocking effect
Prolong QT Interval
Torsades
Ibutilide
Indication
Side Effects
Rapid V Fib
IV only. Torsades
Digitalis Glycosides (Vagotonic)
Digoxin
Digoxin
Mechanism
On Target Effects
Increase vagal nerve acivity, inhibit Na/K pump (Ca overload)
Slows SA Node; Antiarrythmic and arrhthmogenic
Digoxin
Notes
Contraindicated
Side Effects
Causes Ventricular Bigeminy.
Low Therapeutic Window
Wolff Parkinson White
Halo Lights
Adenosine Receptor Agonist
Adenosine
Adenosine
Mechanism
On Target Effects
Notes
Used to terminate acute PSVT by blocking AV node
Rapid half life; given IV
Fixes this or allows attrial flutter diagnosis
HMG-CoA Reductase Inhibitors (Statins)
Lovastatin
Simvastatin
Pravastatin
Atorvastatin
HMG-CoA Reductase Inhibitors (Statins)
Mechanism
Analogs of HMB-CoA that competitively inhibit the enzyme. Liver compensates by increasing number of LDL receptors.
HMG-CoA Reductase Inhibitors (Statins)
On Target Effects
Direct anti-atherosclerotic effects.
HMG-CoA Reductase Inhibitors (Statins)
Notes
Indication
Lowers TG’s
FHCH
HMG-CoA Reductase Inhibitors (Statins)
Contraindicated
Selectivity
Side Effects
Gemfibrozil
CYP3A4; Cleared by liver on 1st pass
CNS, Teratogenic Potential, Rhabdomyolysis , GI
Bile Acid Sequestrants (Resins)
Drugs
Colestipol
Cholestyramine
Colesevelam
Bile Acid Sequestrants (Resins) Mechanism On Target Effects Contraindicated Side Effects
Bind bile acids in intestine and prevent reabsorption
Effects LDL only; Not TG or HDL
Elderly patients and hypertriglyceridema
Prevent absorption of other drugs
Nicotinic Acid- Vitamin B3
Drug
Niacine
Niacine
Mechanism
On Target Effects
Notes
Inhibits mobilization of FFA from adipocytes
Increases HDL by 35% and ApoA1
TG. Effects all
Flushing (aspirin helps) Myocitis
Fibric Acid Derivatives
Drugs
Fenofibrate
Gemifribozil
Fibric Acid Derivatives
Mechanism
On Target Effects
Ligand for the ligand-activated PPAR receptor
Results in increased synthesis by adipose tissue of lipoprotein lipase
Fenofibrate
Indication
Contraindicated
Side Effects
Metabolized by Liver
Gall stones RF
Increased creatinin, pregnancy
Gemifribozil
Notes
Contraindicated
Reduce TG
Gall stones Statins
N-3 Fatty Acids (Fish Oil)
Mechanism
On Target Effects
Reducing SREBP
Reduce TG up to 35%
Penbutolol acts on?
The β1 adrenergic receptors in both the heart and the kidney.
Penbutolol to act as a partial?
Partial agonist proves useful in the prevention of bradycardia.
Penbutolol has also been found to be one of very few compounds that?
Are 5-HT1A antagonists. (Serotonin)
Bisoprolol
Selectivity
Side Effects
B1
Bisoprolol has both lipid and water soluble properties making it a prime candidate over other β-blockers and even over other β1-blockers, being water soluble it will have decreased incidence of CNS side effects
Ezetimibe (prodrug) Mechanism Indication Contraindicated Selectivity
Inhibits transporter mediates GI uptake cholesterol itself (50%)
Lowers plasma cholesterol
Hepatic toxicity if given with a Statin
Bile sequestrants, Biliary excretion;
Ephedrine On Target Effects Notes Selectivity Side Effects
Mainly increase BP through Alpha, but HR/ CO through Beta
Sustaining BP
Mixed acting (D+ID)
Baseball Player; fatal arrhythmias
Milrinone
On Target Effects
Mechanism
Milrinone is a phosphodiesterase 3 inhibitor that works to increase the heart’s contractility.
Phosphodiesterases are enzymes responsible for the breakdown of cAMP
Nesiritide
Mechanism
On Target Effects
The recombinant form of the 32 amino acid human B-type natriuretic peptide.
Counterregulation RAAS
Pindolol
Mechanism
Selectivity
Contraindicated
It possesses ISA (Intrinsic Sympathomimetic Activity). This means that pindolol, particularly in high doses, exerts effects like epinephrine or isoprenaline (increased pulse rate, increased blood pressure, bronchodilation).
Nonselective beta blocker with partial beta-adrenergic receptor agonist activity. Contraindication for hyperthyroidism
Propafenone
Mechanism
Contraindicated
Slows the influx of sodium ions into the cardiac muscle cells, causing a decrease in excitability of the cells.
Hepatic dysfunction, asthma, CHF, or bradycardia.
Ranolazine
Mechanism
Selectivity
Contraindicated
Believed to have its effects via altering the transcellular late sodium current.
Inhibits CYP2D6. Causes toxicity with drugs metabolized by CYP2D6
Contraindicated other medications that increase the QT interval
Furosemide Mechanism On Target Effects Side Effects Contraindicated
Inhibit Na-K-2Cl symporter in TALOH
Copious diuresis with NaCl loss, loss of K+, H+, Ca2+, Mg2+, increase PG’s, venous capacitance; Very protein bound.
Ototoxicity
Interactions with Li+, indomethacin, probenecid, warfarin
Spironolactone
Mechanism
Side Effects
Binds to aldosterone receptor in cytoplasm and prevent its translocation to the nucleus; Reduce Enac channels involved in Na reabsorption.
Hyperkalemia (combine with thiazide); Gynecomastia, hirsutism, uterine bleeding.
Hydrochlorothiazide
Inhibit NaCl reabsorption in the Na+, K+ aldosterone independent segment of D.T.
Low Na, K, Cl, Mg; Hyperuricemia, high Ca, Hyper secretion of renin and aldosterone.
