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### 426 Cards in this Set

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 Km: Definition Km = Substrate at 0.5*Vmax Km reflects the affinity of the enzyme for its substrate Vmax indicates what? Vmax is directly proportional to the enzyme concentration. Relationship between Km and affinity -The lower the Km, the higher the affinity -Smaller Km means enzyme is saturated earlier, which means that small amounts of substrate are picked up by the enzyme. Reading an inverse curve: Y-intercept equals ? 1/Vmax The higher the Y-intercept the lower the Vmax Reading an inverse curve: X-intercept equals ? (1/-Km) The further to the right the x-intercept, the greater the Km Reading an inverse curve: Slope equals ? Km/Vmax Reading an inverse curve: Effect of a competitive inhibitor X-intercept farther to the right, meaning Km is greater, because you need more substrate to get the same effect as the competitive inhibitor is hogging the enzyme. The y-intercept is the same, meaning Vmax hasn't changed, because there isn't any more enzyme. The slope is greater, because Km has increased while Vmax has stayed the same. Reading an inverse curve: Effect of a noncompetitive inhibitor The x-intercept is the same, meaning Km is the same, because the affinity for the enzyme hasn't changed, there's just less of it. The y intercept has increased, meaning Vmax has decreased, because enzyme has been inactivated by the noncompetitive inhibitor The slope is greater, because Vmax has decreased while Km has stayed the same. Competitive inhibitor: Resemble substrate Yes Competitive inhibitor: Overcome by increased substrate? Yes Competitive inhibitor: Binds active site? Yes Competitive inhibitor: Effect on Vmax Unchanged. The amount of enzyme has not changed. Competitive inhibitor: Effect on Km Increased. A lot more substrate needs to be available to seize the active sites. Noncompetitive inhibitor: Resemble substrate? No Noncompetitive inhibitor: Overcome by increased substrate? No Noncompetitive inhibitor: Binds active site? No Noncompetitive inhibitor: Effect on Vmax Decreased. Takes the enzyme out. Noncompetitive inhibitor: Effect on Km Unchanged. Does not change the affinity for the enzyme. Volume of distribution: Abbreviation Vd Vd: Stands for what? Volume of distribution Volume of distribution: definition Vd = (amount of drug in the body)/(plasma drug concentration) Volume of distribution: What alters it? Liver and kidney disease Where are drugs with a low Vd distributed? plasma Where are drugs with a medium Vd distributed? extracellular space Where are drugs with a high Vd distributed? tissues Clearance: definition =(rate of elimination of drug)/(plasma drug concentration) =Vd x Ke where Ke=elimination constant Half life: definition The time required to change the amount of drug in the body by 1/2 during elimination (or during a constant infusion). What percentage of steady state is a drug at after: 1 half life 50% What percentage of steady state is a drug at after: 2 half lives 75% What percentage of steady state is a drug at after: 3 half lives 87.5% What percentage of steady state is a drug at after: 3.3 half lives 90% What percentage of steady state is a drug at after: 4 half lives 94% How many half lives does it take for a drug to reach the following percentage of steady state: 50% 1 half life How many half lives does it take for a drug to reach the following percentage of steady state: 75% 2 half lives How many half lives does it take for a drug to reach the following percentage of steady state: 87.5% 3 half lives How many half lives does it take for a drug to reach the following percentage of steady state: 90% 3.3 half lives How many half lives does it take for a drug to reach the following percentage of steady state: 94% 4 half lives Cp stands for what? target plasma concentration What is the abbreviation for target plasma concentration? Cp In pharmacology, what is F an abbreviation for? Bioavailability What is the abbreviation in pharmacology for bioavailability? F Loading dose: Definition Loading dose = (Cp * Vd)/F (where Cp equals the target plasma concentration, Vd equals volume of distribution, and F equals bioavailability) Maintenance dose: Definition Maintenance dose = (Cp * CL)/F (where Cp is the target plasma concentration and CL is clearance and F is bioavailability) Zero-order elimination: definition Constant elimination over time regardless of drug. How does Cp vary with time during zero-order elimination? Cp decreases linearly with time. Zero-order elimination: Drug examples -Ethanol -Phenytoin -Aspirin (at high concentrations) First-order elimination: definition Rate of elimination is proportional to drug concentration Zero-order elimination vs First-order elimination: Comparison Zero-order: Constant amount of drug eliminated per unit time 1st-order: Constant fraction of drug eliminated per unit time How does Cp vary with time during first-order elimination? Cp decreases exponentially with time. Urine: Which species get trapped in urine? Ionized species In what kind of environment is the following trapped?: Weak acids Basic environments In what kind of environment is the following trapped?: Weak bases Acidic environments In what kind of environment is the following digested?: Weak acids Acidic environments (below pKa) In what kind of environment is the following digested?: Weak bases Basic environments (above pKa) How do you treat an overdose of the following?: Weak acids Bicarbonate How do you treat an overdose of the following?: Weak bases Ammonium chloride Phase I metabolism: Processes Cytochrome P450 -reduction -oxidation -hydrolysis Phase II metabolism: Processes Conjugation -acetylation -glucuronidation -sulfation Phase I metabolism: Metabolites -slightly polar -water-soluble -often still active Phase II metabolism: Metabolites -very polar -renally excreted -inactive What phase of metabolism do geriatric patients lose first? Phase I Effect on dose/effect curve of: competitive antagonist Shifts curve to the right, decreasing potency and increasing EC50. Effect on dose/effect curve of: noncompetitive antagonist Shifts curve downward, decreasing efficacy What is EC50? Dose causing 50% of maximal effect What is Kd? Concentration of drug required to bind 50% of receptor sites How many half lives does it take for a drug to reach the following percentage of steady state: 97% 5 half lives What percentage of steady state is a drug at after: 5 half lives 97% Effect on dose/effect curve: Spare receptors The drug binding and drug effect are independent of each other with effect to the left of binding. This means that EC50 is lower than Kd, so very little drug needs to bind to get 50% of the effect. Effect on dose/effect curve: Partial agonist -Lower maximal efficacy -Potency independent (amount of dose to get to maximum effect) Therapeutic Index: Definition =(TD50)/(ED50) where TD50 equals median toxic dose, and ED50 equals median effective dose. Where are nicotinic receptors found? Preganglionic synapses before: -Cardiac and smooth muscle (Parasympathetic and Sympathetic) -Gland cells (Parasympathetic and Sympathetic) -Nerve terminals (Parasympathetic and Sympathetic) -Renal vascular smooth muscle (Sympathetic) Neuromuscular junctions for skeletal muscle What is the neurotransmitter at Nictoinic receptors? Acetylcholine What is the neurotransmitter at Muscarinic receptors? Acetylcholine Where are muscarinic receptors found? Parasympathetic end plates: -Cardiac and smooth muscle -Gland cells -Nerve terminals Sympathetic end plate: -Sweat glands Where are D1 receptors found? Sympathetic: Renal vascular smooth muscle What type of G-protein is associated with the following receptor type?: alpha-1 Gq What type of G-protein is associated with the following receptor type?: alpha-2 Gi What type of G-protein is associated with the following receptor type?: beta-1 Gs What type of G-protein is associated with the following receptor type?: beta-2 Gs What type of G-protein is associated with the following receptor type?: M1 Gq What type of G-protein is associated with the following receptor type?: M2 Gi What type of G-protein is associated with the following receptor type?: M3 Gq What type of G-protein is associated with the following receptor type?: D1 Gs What type of G-protein is associated with the following receptor type?: D2 Gi What type of G-protein is associated with the following receptor type?: H1 Gq What type of G-protein is associated with the following receptor type?: H2 Gs What type of G-protein is associated with the following receptor type?: V1 Gq What type of G-protein is associated with the following receptor type?: V2 Gs What types of receptors are associated with the following G-proteins: q -alpha-1 -M1 -M3 -H1 -V1 What types of receptors are associated with the following G-proteins: i -alpha-2 -M2 -D2 What types of receptors are associated with the following G-proteins: s -beta-1 -beta-2 -D1 -H2 -V2 What are the major functions of the following receptor type: alpha-1 Increase vascular smooth muscle contraction What are the major functions of the following receptor type: alpha-2 -Decrease sympathetic outflow -Decrease insulin release What are the major functions of the following receptor type: beta-1 -Increase heart rate -Increase contractility -Increase renin release -Increase lipolysis -Increase aqueous humor formation What are the major functions of the following receptor type: beta-2 -Vasodilation -Bronchodilation -Increased glucagon release What are the major functions of the following receptor type: M1 CNS What are the major functions of the following receptor type: M2 Decrease heart rate What are the major functions of the following receptor type: M3 Increase exocrine gland secretions What are the major functions of the following receptor type: D1 Relax renal vascular smooth muscle What are the major functions of the following receptor type: D2 Modulate transmitter release (especially in brain) What are the major functions of the following receptor type: H1 -Increase nasal/bronchial mucus production -Contraction of bronchioles -Pruritus -Pain What are the major functions of the following receptor type: H2 Increased gastric acid secretion What are the major functions of the following receptor type: V1 Increased vascular smooth muscle contraction What are the major functions of the following receptor type: V2 -Increased water permeability and reabsorption in the collecting tubules of the kidney Gq protein pathway -Receptor stimulated -Gq protein stimulates Phospholipase C -Phospholipase C catalyzes the conversion of Lipids to PIP2 -PIP2 splits into IP3 and DAG IP3 stimulates an increase in Calcium concentration DAG activates Protein Kinase C Gs protein pathway -Receptor stimulated -Gs protein stimulates Adenylylcyclase -Adenylylcyclase catalyzes conversion of ATP to cAMP -cAMP activates Protein Kinase A Gi protein pathway -Receptor stimulated -Gi protein inhibits Adenylylcyclase -Decreases conversion of ATP to cAMP -Decreased activation of Protein kinase A Cholinergic pathway (presynaptic events to receptor) 1. Choline transported into presynaptic bulb 2. Acetyl-Coa joints with Choline-ChAT to form acetylcholine, and the two are taken up by a vesicle. 3. The vesicle joins with the cell membrane and ACh is exocytosed 4. ACh is released into the synapse 5. Acetylcholine joints with the Cholinoceptor or is degraded by AChE into Choline + Acetate Hemicholinum: Action and mechanism Inhibits cholinergic transmission Mechanism: Inhibits transfer of choline into presynaptic bulb Vesamicol: Action and mechanism Inhibits cholinergic transmission Mechanism: Inhibits uptake of ACh into a vesicle in the presynaptic bulb Ca2+: Action on presynaptic vesicles Stimulates exocytosis of neurotransmitters from presynaptic bulb Botulinum: Action and mechanism Inhibits cholinergic transmission Mechanism: Inhibits exocytosis of neurotransmitters from presynaptic bulb Noradrenergic pathway (presynaptic events to receptor) 1. Tyrosine is transferred into the presynaptic bulb 2. Tyrosine is converted into DOPA 3. DOPA is converted to Dopamine 4. Dopamine is converted to Norepinephrine and transferred into a vesicle 5. Norepinephrine is exocytosed from the presynaptic terminal 6. 3 possibilities happen a. Norepinephrine binds to a beta adrenoreceptor. b. Norepinephrine is reuptaken by the releasing neuron c. Norepinephrine binds to an alpha-2 receptor on the releasing neuron d. It diffuses away/is metabolized. Metyrosine: Action and mechanism Action: Inhibits noradrenergic transmission Mechanism: Inhibits step where tyrosine is converted into DOPA Reserpine: Action and mechanism Action: Inhibits noradrenergic transmission Mechanism: Prevents sequestration of norepinephrine into vesicles Guanethidine: Action and mechanism Action: Inhibits noradrenergic transmission Mechanism: Inhibits exocytosis of Norepinephrine from presynaptic bulb Amphetamine: Action and mechanism Action: Stimulates noradrenergic transmission Mechanism: Stimulates exocytosis of norepinephrine from presynaptic bulb Tricyclic antidepressant: Mechanism Decreases reuptake of norepinephrine from synaptic cleft into releasing neuron Cocaine: Mechanism Decreases reuptake of norepinephrine from synaptic cleft into releasing neuron Angiotensin II: Effect on noradrenergic pre-synaptic neurons Enhances release of NE Cholinomimetics: Direct agonists Bethanechol, Carbachol, Pilocarpine, Methacholine Cholinomimetics: Indirect agonists Neostigmine (AChE inhibitor), Pyridostigmine, Edrophonium, Physostigmine, Echothiophate Use of: Bethanechol Postoperative and neurogenic ileus and urinary retention Use of: Carbachol -Glaucoma -pupillary contraction -release of intraocular pressure Use of: Pilocarpine Potent stimulator of: -Sweat -Tears -Saliva Use of: Methacholine Challenge test for diagnosis of asthma Use of: Neostigmine AChE inhibitor -Postoperative/neurogenic ileus/urinary retetnion -Myasthenia Gravis -Reversal of neuromuscular junction blockade (postoperative) -No CNS penetration Use of: Pyridostigmine -Myasthenia Gravis (increases strength) -does penetrate CNS Use of: Edrophonium Diagnosis of myasthenia gravis (extremely short acting) Use of: Physostigmine -Glaucoma (crosses blood-brain barrier into CNS) -Atropine overdose Use of: Ecthiophate -Glaucoma Mechanism of indirect cholinomimetics Increase endogenous ACh Synonym for indirect cholinomimetics Anticholinesterases Synonym for anticholinesterases indirect cholinomimetics Bethanechol: mechanism -Activates bowel and bladder smooth muscle -Resistant to AChE Carbachol: mechanism -Contracts ciliary muscle of eye (open angle) -Contracts Pupillary sphincter (narrow angle) -Resistant to AChE Methacholine: mechanism Stimulates muscarinic receptors in airway when inhaled Symptoms of cholinesterase inhibitor poisoning DUMBBELS SAC -Diarrhea -Urination -Miosis -Bronchospasm -Bradycardia -Excitation of skeletal muscle and CNS -Lacrimation -Sweating -Salivation -Abdominal Cramping Antidote to cholinesterase inhibitor poisoning -Atropine (muscarinic antagonist) + -Pralidoxime (chemical antagonist used to regenerate active cholinesterase) Cholinesterase inhibitors -Parathion -Other organophosphates Cholinoreceptor blockers -Atropine (homatropine, tropicamide) -Benztropine -Scopolamine -Ipratropium -Methscoplamine (oxybutin, glycopyrrolate) Cholinoreceptor blockers used to produce: mydriasis and cycloplegia Atropine, homatropine, tropicamide Cholinoreceptor blockers used for: Parkinson's disease Benztropine Cholinoreceptor blockers used for: Motion sickness Scopolamine Cholinoreceptor blockers used for: Obstructive pulmonary disease Ipratropium Cholinoreceptor blockers used for: Genitourinary problems -Methscopolamine -Oxybutin -Glycopyrrolate Application of: Atropine Produce mydriasis and cycloplegia Application of: Homatropine Produce mydriasis and cycloplegia Application of: Tropicamide Produce mydriasis and cycloplegia Application of: Benztropine Parkinson's Disease Application of: Scopolamine Motion sickness Application of: Ipratropium Obstructive pulmonary diseases Application of: Methscopolamine -Reduce urgency in mild cystitis -Reduce bladder spasms Application of: Oxybutin -Reduce urgency in mild cystitis -Reduce bladder spasms Application of: Glycopyrrolate -Reduce urgency in mild cystitis -Reduce bladder spasms Glaucoma drugs: Categories -alpha-agonists -beta-blockers -diuretics -cholinomimetics -prostaglandins Glaucoma drugs - alpha agonists: Epinephrine Brimonidine Which glaucoma drug should not be used in closed-angle glaucoma? Epinephrine Epinephrine: Mechanisms and side effects -M: --Increased outflow of aqueous humor -E: --Mydriasis --Stinging --Do not use in closed angle glaucoma Brimonidine: Mechanisms and side effects M: Decreased aqueous humor synthesis E: No pupillary or vision changes Glaucoma drugs - beta blockers: Timolol Betaxolol Carteolol Glaucoma drugs - beta blockers: Mechanism and side effects M: Decreased aqueous humor secretion E: No pupillary or vision changes Glaucoma drugs - diuretics: Drugs Acetazolamide Glaucoma drugs - diuretics: mechanisms and side effects M: Decreased aqueous humor secretion due to decreased bicarbonate (via inhibition of carbonic anhydrase) E: No pupillary or vision changes Glaucoma drugs - Cholinomimetics: Drugs Direct: Pilocarpine, Carbechol Indirect: Physostigmine, Ecthiopate Glaucoma drugs - Cholinomimetics: Mechanism and Side effects M: -Increase outflow of aqueous humor -Contract ciliary muscle and open trabecular meshwork -Use pilocarpine in emergencies -Very effective at opening canal of Schlemm E: -Miosis -Cyclospasm Glaucoma drugs - Prostaglandins: Drugs Latanoprost (PGF-2alpha) Glaucoma drugs - Prostaglandins: Mechanism and Effects M: Increase outflow of aqueous humor E: Darkens color of iris (browning) Atropine: General effects mnemonic Blocks BUMBLED ASS B: Bradycardia U: Urination M: Miosis B: Bronchospasm L: Lacrimation E: Excitation of skeletal muscle and CNS D: Diarrhea A: Abdominal cramping S: Sweating S: Salivation Atropine: Side effects -Hot as a hare (Increased body temperature; hyperthermia in infants) -Dry as a bone (Dry mouth and dry skin; Urinary retention in men with prostatic hypertrophy; Constipation) -Red as a beet (Flushed skin) -Blind as a bat (Cycloplegia, Acute angle-closure glaucoma in elderly) -Mad as a hatter (disorientation) Atropine: Mechanism Muscarinic antagonist Atropine: Effects on organ system: Eye -Increased pupil dilation -Cycloplegia Atropine: Effects on organ system: Airway -Decreased secretions Atropine: Effects on organ system: Stomach -Decreased acid secretion Atropine: Effects on organ system: Gut -Decreased motility Atropine: Effects on organ system: Bladder -Decreased urgency in cystitis Hexamethonium: Mechanism Nicotinic ACh receptor antagonist: Ganglionic blocker Hexamethonium: Clinical use Prevents vagal reflex responses to changes in blood pressure (eg prevents reflex bradycardia caused by NE) Sympathomimetics: Catecholamines: List -Epinephrine -Norepinephrine -Isoproterenol -Dopamine -Dobutamine Sympathomimetics: Non-catecholamines: List -Amphetamine -Ephedrine -Phenylephrine -Albuterol -terbutaline -Cocaine -Clonidine -Alpha-methyldopa Catecholamines: Epinephrine: Mechanism/selectivity -alpha-1 -alpha-2 -beta-1 (low doses beta-1 selective) -beta-2 Catecholamines: Epinephrine: Applications -Anaphylaxis -Glaucoma (open angle) -Asthma -Hypotension Catecholamines: Norepinephrine: Mechanism/selectivity More selective -alpha-1 -alpha-2 Less selective -beta-1 Catecholamines: Norepinephrine: Applications Hypotension (but decreased renal perfusion) Catecholamines: Isoproterenol: Mechanism/selectivity beta-1 = beta-2 Catecholamines: Isoproterenol: Applications AV block (rare) Catecholamines: Dopamine: Mechanism/selectivity In decreasing order: -D1=D2 -beta -alpha Catecholamines: Dopamine: Applications -Shock (Increased renal perfusion) -Heart failure Catecholamines: Dobutamine: Mechanism/selectivity In decreasing order: -Beta-1 -Beta-2 Catecholamines: Dobutamine: Applications -Shock -Heart failure cardiac stress testing Catecholamines: Amphetamine: Mechanism/selectivity -Indirect general agonist -Releases stored catecholamines Non-catecholamine sympathomimetics: Amphetamine: Applications -Narcolepsy -Obesity -ADD Non-catecholamine sympathomimetics: Ephedrine: Mechanism/selectivity -Indirect general agonist -releases stored catecholamines Non-catecholamine sympathomimetics: Ephedrine: Applications -Nasal decongestion -Urinary incontinence -Hypotension Non-catecholamine sympathomimetics: Phenyephrine: Mechanism/selectivity alpha-1 more than alpha-2 Non-catecholamine sympathomimetics: Phenyephrine: Applications -Pupil dilator -Vasoconstriction -Nasal decongestion Non-catecholamine sympathomimetics: Albuterol: Mechanism/selectivity Beta-2 > Beta-1 Non-catecholamine sympathomimetics: Albuterol: Applications Asthma Non-catecholamine sympathomimetics: Terbutaline: Mechanism/selectivity Beta-2 > Beta-1 Non-catecholamine sympathomimetics: Terbutaline: Applications Asthma Non-catecholamine sympathomimetics: Cocaine: Mechanism/selectivity -Indirect general agonist -Uptake inhibitor Non-catecholamine sympathomimetics: Cocaine: Applications -Vasoconstriction -Local anesthesia Non-catecholamine sympathomimetics: Clonidine: Mechanism/selectivity -Centrally acting alpha-2 agonist -Decreases central adrenergic outflow Non-catecholamine sympathomimetics: alpha-methyldopa: Mechanism/selectivity -Centrally acting alpha-2 agonist -Decreases central adrenergic outflow Non-catecholamine sympathomimetics: Clonidine: Applications Hypertension (especially with renal disease, as there is no decrease in blood flow) Non-catecholamine sympathomimetics: alpha-methyldopa: Applications Hypertension (especially with renal disease, as there is no decrease in blood flow) Sympathomimetics selective for: alpha-1 -Phenylephrine (alpha-1 more than alpha-2) -Norepinephrine (alpha-1 and alpha-2 more than beta-1) Sympathomimetics selective for: alpha-2 -Clonidine -alpha-methyldopa -Norepinephrine (alpha-1 and alpha-2 more than beta-1) -Phenylephrine (alpha-1 more than alpha-2) -Norepinephrine (alpha-1 and alpha-2 more than beta-1) Sympathomimetics selective for: beta-1 -Dobutamine (beta-1 more than beta-2) -Isoproterenol (beta-1 = beta-2) -Epinephrine (at low doses) -Albuterol, terbutaline (beta-2 more than beta-1) Sympathomimetics selective for: beta-2 -Albuterol, terbutaline (beta-2 more than beta-1) -Isoproterenol (beta-1 = beta-2) -Dobutamine (beta-1 more than beta-2) Sympathomimetics selective for: None (general agonists) -Amphetamine -Ephedrine -Cocaine -Epinephrine (alpha and beta) Effect on blood pressure: Norepinephrine Increases from 100 to 150 Mechanism: 1. Stimulates alpha more than beta 2. Systolic blood pressure goes up along with but more than diastolic blood pressure 3. Mean blood pressure rises Effect on blood pressure: Epinephrine Mean pressure stays at 100, with wide pulse-pressure (100) Mechanism: 1. Nonselectively stimulates both alpha and beta receptors 2. Alpha receptors: Systolic blood pressure goes up AND beta receptors: Diastolic blood pressure goes down 3. Mean blood pressure stays the same 4. Pulse pressure is wide Effect on blood pressure: Isoproterenol Mean blood pressure goes down to 50, but pulse-pressure becomes wider (~75). Mechanism: 1. Stimulates beta more than alpha. 2. Diastolic drops along with but more than systolic blood pressure 3. Mean blood pressure drops with wide pulse pressure Effect on heart rate: Norepinephrine 1. Mean pressure goes up 2. Goes down to 50 (reflex bradycardia) Effect on heart rate: Epinephrine 1. Beta-1 receptors are stimulated 2. Increases to 100 Effect on heart rate: Isoproterenol 1. Beta-1 receptors are stimulated more than alpha receptors 2. Increases to ~125 Sympathomimetic of choice for: Anaphylaxis Epinephrine Sympathomimetic of choice for: Open-angle glaucoma Epinephrine Sympathomimetic of choice for: Asthma -Albuterol -Terbutaline -Epinephrine Sympathomimetic of choice for: Hypotension -Epinephrine -Norepinephrine (though with decreased renal perfusion) -Ephedrine Sympathomimetic of choice for: AV block Isoproterenol Sympathomimetic of choice for: Shock -Dopamine (increased renal perfusion) -Dobutamine Sympathomimetic of choice for: Heart failure Dopamine Sympathomimetic of choice for: Heart failure cardiac stress testing Dobutamine Sympathomimetic of choice for: Narcolepsy Amphetamine Sympathomimetic of choice for: Obesity Amphetamine Sympathomimetic of choice for: Attention defecit disorder Amphetamine Sympathomimetic of choice for: Nasal decongestion -Ephedrine -Phenylephrine Sympathomimetic of choice for: Urinary incontinence Ephedrine Sympathomimetic of choice for: Dilation of pupils Phenylephrine Sympathomimetic of choice for: desired vasoconstriction -Phenylephrine -Cocaine Sympathomimetic of choice for: Local anesthesia Cocaine Sympathomimetic of choice for: Treatment of hypertension Clonidine and alpha-methyldopa (especially for those with renal disease, no decrease in blood flow to kidney) alpha-blockers: drug list Non-selective -Irreversible: Phenoxybenzamine -Reversible: Phentolamine alpha-1 selective -Prazosin -Terazosin -Doxazosin alpha-2 selective -Mirtazapine Phenoxybenzamine: Mechanism irreversible nonselective alpha-blocker Phentolamine: Mechanism reversible nonselective alpha-blocker Prazosin: Mechanism alpha-1 blocker Terazosin: Mechanism alpha-1 blocker Doxazosin: Mechanism alpha-1 blocker Mirtazapine: Mechanism alpha-2 blocker Nonselective alpha blockers: Application Pheochromocytoma alpha-2 blockers: Application Depression alpha-1 blockers: Application -Hypertension -Urinary retention in BPH Nonselective alpha blockers: Toxicity -Orthostatic hypotension -Reflex tachycardia alpha-2 blockers: Toxicity -Sedation -Increase in serum cholesterol -Increase in appetite alpha-1 blockers: Toxicity -1st-dose orthostatic hypotension -dizziness -headache Which class of alpha blockers should you use for: Pheochromocytoma Nonselective alpha blockers Which class of alpha blockers should you use for: Hypertension alpha-1 blockers Which class of alpha blockers should you use for: Urinary retention in bph alpha-1 blockers Which class of alpha blockers should you use for: Depression alpha-2 blockers (Mirtazapine) beta-blockers: mechanism in control of: hypertension -decreased cardiac output -decreased renin secretion beta-blockers: mechanism in control of: angina pectoris 1. decreased heart rate and contractility 2. result: decreased O2 consumption beta-blockers: mechanism in control of: MI decrease in mortality (no mechanism given) beta-blockers: mechanism in control of: supraventricular tachycardia decreased AV conduction velocity beta-blockers: mechanism in control of: congestive heart failure slows progression (no mechanism given) beta-blockers: mechanism in control of: glaucoma decreased secretion of aqueous humor which beta-blockers are used in control of: supraventricular tachycardia -Propranolol -Esmolol which beta-blockers are used in control of: glaucoma Timolol beta-blockers: toxicity: non-CV, non-CNS -Impotence -Asthma exacerbation beta-blockers: toxicity: Cardiovascular -bradycardia -AV block -congestive heart failure beta-blockers: toxicity: CNS -sedation -sleep alterations Non-selective beta blockers -Propranol -Timolol -Nadolol -Pindolol (partial agonist) -Labetalol (partial agonist) beta-1-selective beta-blockers A BEAM of beta-1 blockers -Acebutolol (partial agonist) -Betaxolol -Esmolol (short acting) -Atenolol -Metoprolol Antidote for: Acetaminophen N-acetylcysteine Antidote for: Salicylates 1. Alkalinize urine 2. Dialysis Antidote for: Anticholinesterases -Atropine -Pralidoxime Antidote for: Organophosphates -Atropine -Pralidoxime Antidote for: Anti-muscarinic anti-cholinergic agents Physostigmine salicylate Antidote for: beta-blockers Glucagon Antidote for: Digitalis 1. Stop digitalis 2. Normalize potassium 3. Lidocaine 4. anti-digitalis Fab fragments 5. Magnesium Antidote for: Iron Deferoxamine Antidote for: Lead 1st line: CaEDTA & Dimercaprol 2nd line?: Penicillamine Kids: Succimer First Aid lists Penicillamine in the antidotes section, but not in the section below, hence the ? Antidote for: Arsenic -Dimercaprol (BAL) -Succimer -Penicillamine Antidote for: Gold -Dimercaprol (BAL) -Succimer -Penicillamine Antidote for: Mercury -Dimercaprol (BAL) -Succimer Antidote for: Copper Penicillamine Antidote for: Cyanide -Nitrite -Hydroxocobalamin -Thiosulfate Antidote for: Methemoglobin Methylene blue Antidote for: Carbon Monoxide -100% Oxygen -Hyperbaric Oxygen Antidote for: Methanol -Ethanol -Dialysis -Fomepizole Antidote for: Ethylene glycol (antifreeze) -Ethanol -Dialysis -Fomepizole Antidote for: Opioids Naloxone/naltrexone Antidote for: Benzodiazepines Flumazenil Antidote for: Tricyclics NaHCO3 (nonspecific) Antidote for: Heparin Protamine Antidote for: Warfarin -Vitamin K -Fresh frozen plasma Antidote for: tPA Aminocaproic acid Antidote for: streptokinase Aminocaproic acid For what drug(s) is the following an antidote?: N-acetylcysteine Acetaminophen For what drug(s) is the following an antidote?: 1. Alkalinize urine 2. Dialysis Salicylates For what drug(s) is the following an antidote?: Atropine -Anticholinesterases -Organophosphates For what drug(s) is the following an antidote?: Pralidoxime -Anticholinesterases -Organophosphates For what drug(s) is the following an antidote?: Physostigmine salicylate Antimuscarinic, anticholinergic agents For what drug(s) is the following an antidote?: Glucagon beta-blockers For what drug(s) is the following an antidote?: Deferoxamine Iron For what drug(s) is the following an antidote?: CaEDTA Lead For what drug(s) is the following an antidote?: Dimercaprol Dimercaprol is GLAMorous -Gold -Lead -Arsenic -Mercury For what drug(s) is the following an antidote?: Succimer -Lead -Arsenic -Mercury -Gold For what drug(s) is the following an antidote?: Penicillamine -Lead -Copper -Arsenic -Gold For what drug(s) is the following an antidote?: Nitrite Cyanide For what drug(s) is the following an antidote?: Hydroxocobalamin Cyanide For what drug(s) is the following an antidote?: Thiosulfate Cyanide For what drug(s) is the following an antidote?: Methylene blue Methemoglobin For what drug(s) is the following an antidote?: Oxygen Carbon monoxide (Oxygen should be 100% or hyperbaric) For what drug(s) is the following an antidote?: Ethanol -Methanol -Ethylene glycol (antifreeze) For what drug(s) is the following an antidote?: Dialysis -Methanol -Ethylene glycol (antifreeze) -Salicylates For what drug(s) is the following an antidote?: Fomepizole -Methanol -Ethylene glycol (antifreeze) For what drug(s) is the following an antidote?: Naloxone/Naltrexone Opioids For what drug(s) is the following an antidote?: Flumazenil Benzodiazepines For what drug(s) is the following an antidote?: NaHCO3 Tricyclic Antidepressants For what drug(s) is the following an antidote?: Protamine Heparin For what drug(s) is the following an antidote?: Vitamin K Warfarin For what drug(s) is the following an antidote?: Fresh, frozen plasma Warfarin For what drug(s) is the following an antidote?: Aminocaproic acid -tPA -streptokinase Lead poisoning: Signs and symptoms LLEEAADD -Lead Lines on: --gingivae --epiphyses of long bones on x-ray -Encephalopathy -Erythrocyte basophilic stippling -Abdominal colic -sideroblastic Anemia -wrist Drop -foot Drop Lead poisoning: 1st line treatment for adults Both: -Dimercaprol -EDTA Lead poisoning: 1st line treatment for children Succimer (It "sucks" to be a kid who eats lead) Causal agent for the following reaction: Atropine-like side effects Tricyclic Antidepressants Causal agent for the following reaction: Cardiac toxicity -Doxorubicin (Adriamycin) -Daunorubicin Causal agent for the following reaction: Coronary vasospasm Cocaine Causal agent for the following reaction: Cutaneous flushing -Niacin -Ca2+-channel blockers -Adenosine -Vancomycin Causal agent for the following reaction: Torsades des pointes -Class III antiarrhythmics (sotalol) -Class IA antiarrhytmics (quinidine) -Cisapride Causal agent for the following reaction: Agranulocytosis -Clozapine -Carbamazepine -Colchicine Causal agent for the following reaction: Aplastic anemia -Chloramphenicol -Benzene -NSAIDs Causal agent for the following reaction: Gray baby syndrome Chloramphenicol Causal agent for the following reaction: Hemolysis in G6PD-deficient patients G6PD IS PAIN -Isoniazid -Sulfonamides -Primaquine -Aspirin -Ibuprofen -Nitrofurantoin Causal agent for the following reaction: Thrombotic complications oral contraceptive pills Causal agent for the following reaction: Cough ACE inhibitors (not ARBs) Causal agent for the following reaction: Pulmonary fibrosis -Bleomycin -Amiodarone -Busulfan Causal agent for the following reaction: Acute cholestatic hepatitis Macrolides Causal agent for the following reaction: Focal to massive hepatic necrosis -Halothane -Valproic acid -Acetaminophen -Amanita phalloides Causal agent for the following reaction: Hepatitis INH Causal agent for the following reaction: Pseudomembranous colitis -Clindamycin -Ampicillin Causal agent for the following reaction: Adrenocortical insufficiency Glucocorticoid withdrawal (HPA suppression) Causal agent for the following reaction: Gynecomastia Some Drugs Create Extra-Awesome Knockers -Spironolactone -Digitalis -Cimetidine -estrogens -Alcohol (chronic use) -Ketoconazole Causal agent for the following reaction: Hot flashes Tamoxifen Causal agent for the following reaction: Gingival hyperplasia Phenytoin Causal agent for the following reaction: Osteoporosis -Corticosteroids -Heparin Causal agent for the following reaction: Photosensitivity SAT for a photo -Sulfonamides -Amiodarone -Tetracycline Causal agent for the following reaction: SLE-like syndrome (It's not HIPP to have lupus) -Hydralazine -INH -Procainamide -Phenytoin Causal agent for the following reaction: Tendonitis, tendon rupture, and cartilage damage Fluoroquinolones (kids) Causal agent for the following reaction: Fanconi's syndrome Expired tetracycline Causal agent for the following reaction: Interstitial nephritis Methicillin Causal agent for the following reaction: Hemorrhagic cystitis -Cyclophosphamide -Ifosfamide Causal agent for the following reaction: Cinchonism -Quinidine -Quinine Causal agent for the following reaction: Diabetes insipidus -Lithium -Demeclocycline Causal agent for the following reaction: Seizures -Bupropion -Imipenem/cilastatin Causal agent for the following reaction: Tardive dyskinesia Antipsychotics Causal agent for the following reaction: Disulfiram-like reaction -Metronidazole -Certain cephalosporins -Procarbazine -Sulfonylureas Causal agent for the following reaction: Nephrotoxicity/neurotoxicity Polymyxins Causal agent for the following reaction: Nephrotoxicity/ototoxicity -Aminoglycosides -Loop diuretics -Cisplatin P-450 Inducers Queen Barb takes Phen-phen and Strictly Refuses Greasy Carbs -Quinidine (CYP3A4) -Barbiturates -Phenytoin -St. John's Wort -Rifampin -Griseofulvin -Carbamazepine P-450 Inhibitors Inhibitors Quickly Stop Cyber-Kids from Eating Grapefruit -Isoniazid -Quinidine (CYP2D6) -Sulfonamides -Cimetidine -Ketoconazole -Erythromycin -Grapefruit juice P-450 inducer or inhibitor: Quinidine Inhibitor: CYP2D6 (more prominent) Inducer: CYP3A4 P-450 inducer or inhibitor: Barbiturates Inducer P-450 inducer or inhibitor: Phenytoin Inducer P-450 inducer or inhibitor: Rifampin Inducer P-450 inducer or inhibitor: Griseofulvin Inducer P-450 inducer or inhibitor: Carbamazepine Inducer P-450 inducer or inhibitor: St. John's wort Inducer P-450 inducer or inhibitor: Isoniazid Inhibitor P-450 inducer or inhibitor: Sulfonamides Inhibitor P-450 inducer or inhibitor: Cimetidine Inhibitor P-450 inducer or inhibitor: Ketoconazole Inhibitor P-450 inducer or inhibitor: Erythromycin Inhibitor P-450 inducer or inhibitor: Grapefruit juice Inhibitor Active metabolite of ethylene glycol Oxalic acid Active metabolite of methanol -Formaldehyde -Formic acid Active metabolite of ethanol Acetaldehyde Pathway and toxicities of metabolism of: ethylene glycol 1. Ethylene glycol is converted by alcohol dehydrogenase to 2. Oxalic acid causes: -Acidosis -Nephrotoxicity Pathway and toxicities of metabolism of: methanol 1. Methanol is converted by alcohol dehydrogenase to 2. Formaldehyde and formic acid which cause: -Severe Acidosis -Retinal damage Pathway and toxicities of metabolism of: ethanol 1. Ethanol is converted by alcohol dehydrogenase to 2. Acetaldehyde which causes: -Nausea -Vomiting -Headache -Hypotension What enzyme is inhibited by disulfiram? Acetaldehyde dehydrogenase What inhibits acetaldehyde dehydrogenase? Disulfiram Clinical uses/toxicities for: Echinacea Use: Common cold Toxicities: -GI distress -dizziness -headache Clinical uses/toxicities for: Ephedra Uses: As for ephedrine Toxicities: -CNS and cardiovascular stimulation At high doses: -Arrhythmias -Stroke -Seizure Clinical uses/toxicities for: Feverfew Use: Migraine Toxicities: -GI distress -Mouth ulcers -Antiplatelet actions Clinical uses/toxicities for: Ginkgo Use: Intermittent claudication Toxicities: -GI distress -anxiety -insomnia -headache -antiplatelet actions Clinical uses/toxicities for: Kava Use: Chronic anxiety Toxicities: -GI distress -sedation -ataxia -hepatotoxicity -phototoxicity -dermatotoxicity Clinical uses/toxicities for: Milk thistle Use: Viral hepatitis Toxicities: Loose stools Clinical uses/toxicities for: Saw palmetto Use: Benign prostatic hyperplasia Toxicities: -GI distress -Decreased libido -Hypertension Clinical uses/toxicities for: St. John's wort Use: Mild to moderate depression Toxicities: -GI distress and phototoxicity -serotonin syndrome with SSRIs -induces P-450 system Clinical uses/toxicities for: DHEA Uses: Symptomatic improvement in females with SLE or AIDS Toxicities: -Androgenization (premenopausal women) -Estrogenic effects (post menopausal) -Feminization (young men) Clinical uses/toxicities for: Melatonin Use: -Jet lag -Insomnia Toxicities: -Sedation -Suppresses midcycle LH -Hypoprolactinemia Category for drug names ending with: -afil Erectile dysfunction (eg Sildenafil) Category for drug names ending with: -ane Inhalational general anesthetic (eg Halothane) Category for drug names ending with: -azepam Benzodiazepine (eg Diazepam) Category for drug names ending with: -azine Phenothiazine (neuroleptic, antiemetic) (eg Chlorpromazine) Category for drug names ending with: -azole Antifungal (eg Ketoconazole) Category for drug names ending with: -barbital Barbiturate (eg Phenobarbital) Category for drug names ending with: -caine Local anesthetic (eg Lidocaine) Category for drug names ending with: -cillin Penicillin (eg Methicillin) Category for drug names ending with: -cycline Antibiotic, protein synthesis inhibitor (Tetracycline) Category for drug names ending with: -ipramine Tricyclic Antidepressant (eg Imipramine) Category for drug names ending with: -navir Protease inhibitor (eg Saquinavir) Category for drug names ending with: -olol beta-blocker (eg Propranolol) Category for drug names ending with: -operidol Butyrophone (neuroleptic) (eg Haloperidol) Category for drug names ending with: -oxin Cardiac glycoside (inotropic agent) (eg Digoxin) Category for drug names ending with: -phylline Methylxanthine (eg Theophylline) Category for drug names ending with: -pril ACE inhibitor (eg Captopril) Category for drug names ending with: -terol beta-2 agonist (eg Albuterol) Category for drug names ending with: -tidine H2 antagonist (eg Cimetidine) Category for drug names ending with: -triptyline Tricyclic antidepressant (eg Amitryptyline) Category for drug names ending with: -tropin Pituitary hormone (eg Somatotropin) Category for drug names ending with: -zosin alpha-1 antagonist (eg Prazosin) Common ending for drug names in the following category: Erectile dysfunction -afil (eg Slidenafil) Common ending for drug names in the following category: Inhalational general anesthetic -ane (eg Halothane) Common ending for drug names in the following category: Benzodiazepine -azepam (eg Diazepam) Common ending for drug names in the following category: Phenothiazine (neuroleptic, antiemetic) -azine (eg Chlorpromazine) Common ending for drug names in the following category: Antifungal -azole (eg Ketoconazole) Common ending for drug names in the following category: Barbiturate -barbital (eg Phenobarbital) Common ending for drug names in the following category: Local anesthetic -caine (eg Lidocaine) Common ending for drug names in the following category: Penicillin -cillin (eg Methicillin) Common ending for drug names in the following category: Bacterial protein synthesis inhibitor -cycline (eg Tetracycline) Common ending for drug names in the following category: Tricyclic antidepressant -ipramine (Imipramine) -triptyline (Amitriptyline) Common ending for drug names in the following category: Protease inhibitor -navir (Saquinavir) (Mnemonic: Navir tease a pro) Common ending for drug names in the following category: beta-antagonist -olol (Propranolol) Common ending for drug names in the following category: butyrophenone (neuroleptic) -operidol (Haloperidol) Common ending for drug names in the following category: Cardiac glycoside -oxin (Digoxin) Common ending for drug names in the following category: Methylxanthine -phylline (eg Theophylline) Common ending for drug names in the following category: ACE inhibitor -pril (Captopril) Common ending for drug names in the following category: beta-2 agonist -terol (eg Albuterol) Common ending for drug names in the following category: H2 antagonist -tidine (eg Cimetidine) Common ending for drug names in the following category: Pituitary hormone -tropin (eg Somatotropin) Common ending for drug names in the following category: alpha-1 antagonist -zosin (eg Prazosin)