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Cardiology Drugs
Drugs for Cardiology
Drug (generic) | Class | Receptor | Effect | Use |
---|---|---|---|---|
Norepinephirne | natural catecholamine; direct acting | B1 agonist, alpha agonist, no affinity for B2 | increases cardiac contractility; arterial and vasoconstrictor; reduces renal perfusion; minor effect on splanchnic blood flow | Temporary therapeutic use in severe hypotension that is non-responsive to other sympathomiemetics; give only via central venous catheter (tissue toxicity) |
Dopamine | natural catecholamine, mixed sympathomiemetic | D1 receptor in periphery | Low dose (D1): increase NE; more splanchnic and cerebral flow + coronary renal perfusion. Mid (beta adrenergic): more cardiac contractility) no/minor effect on BP + HR. High: alpha-1 receptors (increased BP, vasoconstriction of organs, tachycardia) | Severe congestive heart failure, especially in patients with oliguria and low or normal peripheral vascular resistance |
Isoproterenol | Synthetic sympathomimetic amine; direct adrenergic agonist | Non selective B agonist (B1>B2) | Chronotropic effects (increases HR and AV conduction) and ionotropic (increases cardiac contractility and cardiac output); increases myocardial O2 demand; peripheral vasodilation and decreases diastolic pressure | When myocardium poorly contractile and HR slow yet MAP high: after cardiac surgery or patients with prior Beta-blockade (or overdose); bronchodiolator; Avoid in cases of myocardial ischemia (increases O2 demand) |
Dobutamine | Selective beta adrenergic receptor | B1>B2>>alpha (no dopaminergic effects) | Increases cardiac contractility and HR; mild increase in vasodilation; no direct effects on renal or splanchnic blood flow; more prominent ionotropic than chronotropic effects, minimal effects on myocardial oxygen demand | (Similar to isoproterenol, though ok for ischemic hearts) When myocardium poorly contractile and HR slow yet MAP high: after cardiac surgery or patients with prior Beta-blockade (or overdose); bronchodiolator |
Terbutaline | Selective B2 adrenergic receptor agonists | B2 | bronchodilators | Short acting asthma and chronic obstructive pulmonary disease |
Albuterol | Selective B2 adrenergic receptor agonists | B2 | bronchodilators | Short acting asthma and chronic obstructive pulmonary disease |
Salmeterol | Selective B2 adrenergic receptor agonists | B2 | bronchodilators | Long acting asthma and chronic obstructive pulmonary disease |
Formeterol | B2 | |||
Arformoterol | B2 | bronchodilators | ||
Ritodrine | Tocolytic agent (B2 adrenergic receptor agonist for premature labor); phenethylamine derivative | B2 adrenergic in myometrial cells in uterus | Dreceases intensity and frequency of uterine contractions via adenyl cyclase-->increase cAMP-->enhances Ca++ efflux from SM cells--> prevents contractions | Used to control premature labor; does not prevent pre-term labor |
Phenylephrine | alpha-1 adrenergic agonist | alpha-1 receptors, but also activates B receptors at much higher concentrations | Arterial vasoconstriction during IV infusion | Nasal and opthalmic formulations used as mydriatics or decongestants |
Naphozoline, phenylephirine | Occular vasoconstrictor decongestant; alpha receptor agonist | alpha-receptor | reduces hyperemia in eye | for eyes in people with allergies; can differentiate between ciliary and conjunctival infection (ciliary infection does not result in loss of redness when alpha agonist used) |
Oxymetazoline | Nasal vasoconstrictor-decongenstant (alpha-1 receptor adrenergic agonist) | alpha 1 | vasoconstriction + reduces blood flow and mucosa swelling | Relieve nasal discomfort in colds, allergies, and hay fever; relieve sinus congestion and pressure. Prolonged use-->rebound phenomemon and mucosa necrosis |
Modafinil, ardafinil | alpha-1 adrenergic agonists with central effects | alpha-1 adrenergic receptors in CNS | psychostimulants; increases vigilance; decreases need for sleep; similar effects as indirect-acting sympathomimetics; hypothalamic histamine release | in eldery: treat vigilance and attention disorders. Adverse effects: agitation, excitation, aggressiveness. Narcolepsy, shift work, sleep disorder, excessive daytime sleepiness |
clonidine | prototypic selective alpha-2 central adrenergic agonist | alpha-2 receptor in vasomotor center (rostral ventrolateral medulla (RVLM)) | alpha-2 receptors in RVLM inhibit sympathetic outflow + vasomotor tone; decreases norepinephrine release in prejunctional alpha-2 receptors | Antihypertensive drug |
alpha-methyldopa | prototypic selective alpha-2 central adrenergic agonist | alpha-2 receptor in vasomotor center (rostral ventrolateral medulla (RVLM)) | alpha-2 receptors in RVLM inhibit sympathetic outflow + vasomotor tone; decreases norepinephrine release in prejunctional alpha-2 receptors | Antihypertensive drug |
guanfacine | prototypic selective alpha-2 central adrenergic agonist | alpha-2 receptor in vasomotor center (rostral ventrolateral medulla (RVLM)) | alpha-2 receptors in RVLM inhibit sympathetic outflow + vasomotor tone; decreases norepinephrine release in prejunctional alpha-2 receptors | Antihypertensive drug |
Guanabenz | prototypic selective alpha-2 central adrenergic agonist | alpha-2 receptor in vasomotor center (rostral ventrolateral medulla (RVLM)) | alpha-2 receptors in RVLM inhibit sympathetic outflow + vasomotor tone; decreases norepinephrine release in prejunctional alpha-2 receptors | Antihypertensive drug |
Amphetamine (and dextro-amphetamine) | Indirectly-acting sympathomimetic | None--increases monoamine release (NE, DA, 5HT), which bind to their receptors | Powerful CNS stimulant (dextro amphetamine is more potent) | ADHD, narcolepsy, and suppression of appetite |
Metamphetamine (and methamphetamine hydrochloride) | Indirect acting sympathomimetics; manufactured from pseudoephedrine | None--increases monoamine release (NE, DA, 5HT), which bind to their receptors | Mainly central effects; stimulant; similar to cocaine | Side effects: tachycardia, hypertension, hyperthermia, cerebrovascular incidents, and myocardial infarction; may induce sympathomimetic toxicity |
Ephedrine | alkaloid; mixed-acting sympathomimetic | agonist for both alpha and beta receptor; also enhances NE release | mixed acting sympathomimetic drug (pan receptor agonist) | enhances weight loss, but causes cardiovascular toxicity and mortality |
Methylphenidate (ritalin) | indirect acting sympathomimetic | None (?); inhibits the reuptake of NE and DA and stimulates cerebral cortex similar to amphetamines | blocks reuptake of NE and DA in CNS | ADHD |
Dexamphetamine (Dexedrin) | indirect acting sympathomimetic | None (?); inhibits the reuptake of NE and DA and stimulates cerebral cortex similar to amphetamines | Completely inhibits catecholamine reuptake by presynaptic nerve terminal | ADHD |
Bupoprion (wellbutrin) | indirect acting sympathomimetic | None (?); inhibits the reuptake of NE and DA and stimulates cerebral cortex similar to amphetamines | inhibits neuronal NE and DA reuptake by presynaptic nerve terminal | ADHD |
Atomoxetine | indirect acting sympathomimetic | None (?); inhibits the reuptake of NE and DA and stimulates cerebral cortex similar to amphetamines | selectively inhibits neuronal NE (not DA?) reuptake by presynaptic terminal | ADHD |
Prazosin, doxazosin, terazosin | alpha-1 selective adrenergic antagonists | alpha1A, 1B, 1D | Inhibits vasoconstriction-->vasodilation in resistant arteriolar vessels and veins --> fall in blood pressure due to less MAP and reduced venous return; effect depends on activity of sympathetic nervous system | Used against hypertension |
Alfuzosin, tamsulosin, silodosin | alpha-1 selective adrenergic antagonists | alpha 1A (1D) > 1B | Inhibits vasoconstriction-->vasodilation in resistant arteriolar vessels and veins --> fall in blood pressure due to less MAP and reduced venous return; effect depends on activity of sympathetic nervous system | Used in benign prostatic hyperplasia (BPH) due to higher number of alpha-1A receptors; alpha-1B, D receptors still activated, but effects not seen as much |
Yohimbe | selective alpha-2 adrenergic antagonist | alpha-2 (mainly in CNS) | increases blood pressure via central mechanism (opposite of clonidine) by inhibiting alpha-2 receptors in CNS-->increased sympathetic outflow | only used in veterinarian medicine |
Phenoxibenzamine, phentolamine | old, classical non-selective alpha-adrenergic antagonists | alpha-receptor antagonists | antihypertensives; Phenoxibenzamine is irreversible antagonist; phentolamine is competitive antagonist | limited clinical use: preoperative pheochromocytoma, adrenergic crisis, frost bite, prevention of dermal necrosis, sympathomimetic extravasation |
Ergotamine, ergonovin, bromocriptin | Ergot alkaloids | Many alpha-receptor agonists, weak dopamine receptor agonist, or serotonin receptor antagonist/partial agonist | various (depends if antagonist or agonist) | Ergotamine: migraine; ergonovin: prevents postpartum hemorrhage. Bromocriptin (DA agonist): parkinsonism and control prolactin |
Epinephrine | natural catecholamine, direct acting agonist | alpha and beta adrenergic receptors; at low dose, D1; at mid dose, beta adrenergic; at high dose, alpha-1 adrenergic | Direct agonist of receptor; response depends on relative ratio of receptors, penetration, concentration at site of action, sensitivity of adrenergic receptors, and level of activation | Cardiac arrest (increases systemic vascular rsistance, diastolic blood pressure, decreases non-vital organ perfusion. CPR, anaphylactic shock, asthma, glaucoma, local anesthetics (prolongs effects) |