Drugs Flashcards
Albuterol
Beta 2; asthma
Clonidine
A2; HTN
Dobutamine
B1; Cardiogenic shock
Dopamine
D; vasodilation, vasoconstriction, cardiac
Epinephrine
A/B1&2; Hypotension
Isoproteronol
B1/2; Cardiac
Norepinephrine
Some A/B1>2; (cardiac)
Direct acting Adrenergic agonists (7)
- Albuterol
- Clonidine
- Dobutamine
- Dopamine
- Epinephrine
- Isoproterenol
- Norepinephrine
Indirect acting adrenergic agonist (1)
- Amphetamine
Amphetamine
Displaces NE, reversed NET and blocks DAT
Direct & Indirect acting Adrenergic Agonists (1)
- Ephedrine
Ephedrine
Direct - mimics epinephrine
Indirect - release of catecholamines
*CAN cross BBB
Neurotransmitter Classes (6)
- Esters
- Monoamines
- Amino acids
- Purines
- Peptides
- Inorganic gases (not stores; released as needed)
Esters (1)
- Acetylcholine (CHOLINERGIC)
Monoamines (3)
- Norepinephrine
- Serotonin
- Dopamine
Amino acids (2)
- Glutamate (E)
- GABA (I)
Purines (2)
- Adenosine
- ATP
Peptides (2)
- Substance P
- Endorphins
Inorganic gases (1)
- Nitric oxide
Catecholamines (5)
- Epi
- Norepi
- Isoproterenol
- Dopamine
- Dobutamine
Adrenoceptor Antagonist Drugs (5 - Reversible and Irreversible)
- Phentolamine
- Tolazolin
- Prazosin
- Labetolol
- Phenoxybenzamine
Reversible/Competitive adrenoceptor antagonists (4) and use
- Phentolamine
- Tolazolin
- Prazosin
- Labetalol
*Used for hypertension related to pheochromocytoma
Irreversible/non-competitive adrenoceptor antagonist (1)
- Phenoxybenzamine
What receptor do adrenoceptor antagonists bind to?
Alpha receptors
What 2 things do beta agonists do to the heart?
- Negative inotrope (force)
- Negative chronotrope (rate)
What 3 things do beta agonists do to the blood vessels?
- Oppose B2 mediated vasodilation
- Acute: inc. peripheral resistance
- Chronic: dec. peripheral resistance (mechanism unclear)
What are the 4 beta-antagonist drugs?
- Propranolol (Inderal)
- Metoprolol (Lopressor)
- Atenolol (Ternormin)
- Esmolol
Propranolol (Inderal)
Beta 1 & 2 receptors
Metoprolol (Lopressor) and Atenolol (Tenormin)
Mainly A1 selective; safer in COPD/diabetic patients
Esmolol
ultra-short acting (given in OR); B1 selective
Indirect-acting cholinomimetics (4)
- Edrophonium
- Carbamates
- Neostigmine
- Organophosphates
Indirect-acting cholinomimetics (Simple alcohols)
- Edrophonium
Indirect-acting cholinomimetics (Carbamic acid esters of alcohols)
- Carbamates
- Neostigmine
Indirect-acting cholinomimetics (Organic derivatives of phosphoric acid)
- Organophosphates
Major uses of cholinomimetics (4)
- Disease of the eye
- GI and urinary tracts
- NMJ - MYASTHENIA GRAVIS
- Atropine OD
S/S to look for with organophosphate exposures
SLUDGE-M
Salivation, Lacrimation, Urination, Defecation, GI Motility, Emesis, Miosis (constricted pupil)
S/S of poisonous mushrooms (Muscarinic excess)
SLUDGE-M
Salivation, Lacrimation, Urination, Defecation, GI Motility, Emesis, Miosis (constricted pupil)
S/S of atropine OD (belladona plant)
BRAND
Blind, red, absent bowel sounds, nuts, dry
Treatment of organophosphate exposure
Atropine
Pralidoxime
Tx of poisonous mushrooms/muscarinic excess
Atropine
Tx of atropine OD
Physostigmine
NO, Nitrates, Nitrites
Activate guanylate cyclase - inc cGMP
RELAXATION
Beta-2 agonists (vascular smooth mm)
GPCR-cAMP
RELAXATION (MAINLY RESPIRATORY)
Beta blockers (smooth mm)
Decrease demand on the heart
Ca Channel blockers (smooth mm)
Less total calcium
RELAXATION
Sildenafil
Blocks PDE5 - inc. cGMP
RELAXATION
Ca Channel blockers (3)
- Dihydropyridines
- Verapamil
- Diltiazem
Dihydropyridines (selectivity)
Peripheral vasculature
Verapamil and Diltiazem (selectivity)
Cardiac
Antihypertensive Agents (4)
- Diuretics
- Sympathoplegics (alpha/beta blockers)
- Direct vasodilators
- Anti-angiotensins
Diuretics MOA
deplete sodium and water
Sympathoplegics (alpha/beta blockers) MOA
decrease PVR, recude CO
Direct vasodilators MOA
relax vascular smooth mm
Anti-angiotensins MOA
block activity/production
CNS sympathoplegics (2)
- Methyldopa
- Clonidine
Adrenoceptor Antagonist (6)
- Propanolol
- Metoprolol
- Atenolol
- Prazosin
- Terazosin
- Doxazosin
Clonidine & Methyldopa
PRIMARY anti-HTN d/t alpha agonist activity in brainstem = dec. sympathetic stimulation
BINDS MORE TIGHTLY TO A2 THAN A1
Propranolol
Lowers BP; prevents reflex tachycardia
Antagonizes B1/2 receptors
Dec. CO
Inhibits renin production
toxicity associated w/ beta-blockade
Prazosin, Terazosin, Doxazosin
A1 blockers in arterioles/venules
Dilates both resistance and capacitance vessels
BP I reduced more in an upright position
Minoxidil
Vasodilator - opens K+ channels in smooth mm
Dilates arteries/arterioles
Hydralazine
Dilates arterioles (NO production)
Hydralazine toxicities
HA/N/Sweating/Flushing
Sodium Nitroprusside
HTN emergencies/cardiac failure
dilates arterial and venous vessels
Relaxes vascular smooth mm - breaks down in blood to release NO and inc. cGMP
Fenoldopam
Peripheral arteriolar dilator
HTN emergencies/post-op HTN
AGONIST OF D1 receptors
Digoxin
Inhibits Na/K/ATPase
maintains normal resting potential
+ inotrope (force)
Can have hyperkalemia and calcemia or hypomagnesemia
Digoxin toxicity (EC50 & TC50)
EC50 = 1 ng/ml
TC50 = 2 ng/ml
Digoxin effects on other organs
It affects ALL EXCITABLE tissue
Inhibition of Na/K/ATPase (smooth mm, CNS)
Phosphodiesterase inhibitors (1)/MOA
Milrinone (PARENTERAL ONLY)
block PDE3 enzyme which inactivates cAMP and cGMP
+ inotropic effects
Antiarrythmic Agents (4/5 classes)
- Sodium channel blockade (-caines)
- Sympatholytic (Beta blockers)
- Prolong action potential duration (other mechanisms besides sodium channels) = Amiloride
- Block cardiac calcium channel currents (Verapamil)
- OTHER
Sodium channel blockers (3)
- Quinidine
- Lidocaine
- Flecainide
Carbonic Anhydrase inhibitors
Acetazolamide
Loop diuretics (2)
- Furosemide (sulfanamide)
- Ethacrynic acid
Thiazides
Work in distal convoluted tubule and inhibit NCC
1. Hydrochlorothiazides
2. Sulfonamides
Aldosterone
Inc. Na/water reuptake ENAC
inc. blood volume
Potassium-sparing diuretics
- Spironolactone
ADH/Vasopressin
inc. water reabsorption
adds AQP2 to apical membrane
inc. blood volume
ADH/Vaso antagonist
Conivaptan
Osmotic Diuretics
Mannitol
Diphenhydramine
H1 antihistamine
H1 uses
- Sedation
- Antinausea/antiemetic
- Antiparkinsonism
- Local anesthesia
H2 uses
Not as effective as PPIs
Drugs used in asthma (3)
- Bronchodilators
- Anti-inflammatory agents
- Leukotriene antagonists
Bronchodilators - for asthma (3)
- Beta-agonists
- Antimuscarinics
- Methylxanthines
Anti-inflammatory agents - for asthma (3)
- Steroids
- Antibodies
- Alow anti-inflammatory drugs
Leukotriene antagonists (2)
- Lipoxygenase inhibitors
- Receptor inhibitors
Sympathomimetics (5)
- Epi
- Isoproterenol
- Terbutaline
- Formoterol
- Salmeterol
Muscarinic Antagonists (3)
- Atropine
- Ipratropium bromide (COPD)
- Tiotropium (COPD) - 24 hour
Zileuton
Inhibits 5-lipoxygenase
Zafirlukast/Montelukast
Inhibits binding to leukotriene pathway receptor
Omalizumab (Xolair)
Anti-IgE monoclonal antibody - targets portion that binds to mast cells
Lessens asthma severity
Decreases corticosteroid requirement
Reduced hospitalizations
Buspirone
5-HT1A agonist
Anxiolytic, OCD
Triptans
5-HT1D/B agonist
Migraines/HA
Toxicity of Triptans
Recurrence of migraine
Serotonin syndrome
What 3 drugs can cause serotonin syndrome
- Triptans
- SSRIs
- MAOIs
Phenoxybenzamine
5-HT2 antagonist
Carcinoid tumors
Cyproheptadine
cold induced urticaria
Ondansetron
5-HT3 antagonist
Serotonin syndrome tx
Sedation (benzos), intubation/ventilation
Neuroleptic malignant syndrome tx
Diphenhydramine
Malignant hyperthermia tx
Dantrolene
Antidepressant treatments (4 classes)
- SSRIs
- SNRIs
- TCAs
- MAOIs
Elavil
TCAs
Inhibits SERT, NET and anticholinergic
Prozac/Zoloft
SSRIs
Inhibit SERT
Pristique/Cymbalta
SNRI’s (SERT/NET)
Ethoxusimide
Absence seizures
Vigabatrin
infantile spasms
Lamotrigine (Lamictal)
Focal/partial seizures
Phenytoin/Phenobarb/Carbamazepine
Partial seizures and general tonic-clonic
Valproic acid
Absence, tonic, atonic, clonic