pharma Flashcards
Difference between Pharmacokinetics and Pharmacodynamics
Pharmacokinetics - actions of the body on the drug. Pharmacodynamics - actions of the drug on the body.
Heparin is the anticoagulant used for pregnancy due to its large size (unable to cross the placenta). What is it’s MOA?
Increases antithrombin III, monitored using PTT, antidote is Protamine Sulfate
Which quadrant of the buttocks is the safest for IM drug administration?
Superolateral
What is drug is contraindicated to be given via IM?
Anticoagulants - may cause hematomas
Through which BV do drugs administered SL pass before reaching the heart?
Lingual vein > IJV > Brachiocephalic/Innominate vein > SVC > RA
Route that has partial avoidance of the first pass effect
Rectal or Suppository route
DOC for Parkinsons
Levodopa - Dopamine will not cross the BBB
Acidic drugs bind to Albumin, Basic drugs bind to?
Orosomucoid
DOC for biolar disorder
Lithium
Antiemetic that is contraindicated for patients with seizures
Meperidine - active metabolite Normeperidine exacerbates seizures
Cholinergic antagonist used in the treatment of Parkinson’s disease
Benztropine - reduces tremors
Colinergic antagonist, applied as a transdermal patch, used for motion sickness
Scopolamine - antagonizes histamine and serotonin
Competitively blocks Nn nicotinic Ach receptors. Used for hypertensive emergencies. SE of postural HTN.
Hexamethonium
Drugs that are important for producing complete skeletal muscle relaxation in surgery
Neuromuscular blockers
Norepinehrine comes from what AA?
Tyrosine
Sympathomimetic (non-selective, direct acting). Last resort drug for cardiogenic shock
Norepinephrine
Non-selective, direct acting sympathomimetic used for shock and heart failure
Dopamine
Beta non selective sympathomimetic used for asthma
Isoproterenol
Treatment for rebound hypertension caused by Clonidine
Phentolamine
Alpha 2 selective sympathomimetic for the treatment of Pre-eclampsia
Methyldopa - decreases central sympathetic outflow
Alpha 2 selective sympathomimetic that decreases secretion of aqueous humor
Apraclonidine (Brimonidine) - for glaucoma
Beta 1 selective sympathomimetic used to treat acute heart failure
Dobutamine - may also be used in cardiac stress testing
Beta 2 selective sympathomimetic, DOC for acute asthma attacks
Albuterol/Salbutamol
Beta 2 selective sympathomimetic that is used for tocolysis of preterm labor
Terbutaline and Ritodrine
Drug used for Pheochromocytoma (pre-surgical)
Phenoxybenzamine - alpha non selective, irreversible adrenergic antagonist
Alpha 1 selective adrenergic antagonist that is most selective for prostatic smooth muscle
Tamsulosin (Prazosin)
SE of Propanolol
Masks symptoms of hypglycemia in diabetics
Non selective beta blocker (adrenergic antagonist) with the longest half life
Nadolol
Selective B1 blocker (adrenergic antagonist) used for supraventricular tachycardia
Esmolol - also has the shortest half life
Muscle that controls accommodation of the eye
Ciliary muscle (parasympathetic)
Prostaglandin that increases outflow through Canal of Schlemm
Latanoprost
Diuretic that inhibits Na/Cl transporter in distal convoluted tubule
Hydrochlorothiazide
Loop diuretic that inhibits Na/K/Cl transporter in the thick ascending limb of the Loop of Henle
Furosemide
Obsolete drug for HTN, may cause suicidal ideation
Reserpine - nerve terminal blocker
3 drugs used to control HTN in pheochromocyta
Phenoxybenzamine, Phentolamine, Labetalol
DOC for heart failure in African patients. May also be used for pre-eclampsia
Hydralazine
Marker for drug induced lupus
Anti-histone antibodies
Vasodilator for HTN and alopecia
Minoxidil - can cause hypertrichosis or excessive hair growth
Block voltage gated L type calcium channels in the heart. For supraventricular tachycardia. Has a side effect of gingival hyperplasia
Verapamil (Diltiazem)
Vasodilator that may cause cyanide toxicity
Nitroprusside
Most common cause of bradykinin induced cough. Also delays progression of diabetic nephropathy
Captopril - ACE inhibitor
Hyperkalemia and ACE inhibitors/ARBs
Drugs reduce aldosterone levels and cause potassium retention
Renin antagonist. Drug for HTN
Aliskiren
DOC for Prinzmetal’s angina
CCB - Diltiazem
Why are antilipid drugs given to patients with unstable angina?
Statins stabilize the plaques
Which portion of the ETC is affected by cyanide poisoning?
Complex IV (cytochrome oxidase)
Antidote for cyanide poisoning
Inhaled amyl nitrite + IV sodium nitrite + IV sodium thiosulfate
Short acting nitrate that affects veins more
Nitroglycerin
Nitrate induced headache
Meningeal artery vasodilation
Non-dihydropyridine CCB used to treat angina and Raynaud’s phenemenon
Diltiazem
Beta blocker that has erectile dysfunction as a side effect
Propanolol
Cardiac glycoside with a narrow therapeutic index
Digoxin - inhibits Na/K ATPase, increasing intracellular Ca, drug for heart failure with systolic dysfunction
DOC in antiarrhythmic treatment of digitalis toxicity
Lidocaine
Digitalis toxicity is increased by:
Hypokalemia, hypomagnesemia, and hypercalcemia
These drugs are of no value in CHF
Calcium channel blockers
Diuretic that can be used for immediate reduction of pulmonary congestion and severe edema in HF
Furosemide (loop diuretic)
These drugs reduce progression of heart failure
Beta blockers - Carvedilol, Labetolol and Metoprolol
Condition induced by antiarrhythmics where there is polymorphic ventricular tachycardia on ECG
Torsades de pointes
Class 1 antiarrhythmic with Lupus like syndrome as a side effect
Procainamide - used especially after an MI
Class 1 antiarrhythmic that can cause marked antimuscarinic effects
Disopyramide
Class 1 antiarrhythmic that can also be used for malaria. SEs of cinchonism and autoimmune reactions (ITP)
Quinidine
Drug for class 1A antiarrhythmics to reverse drug induced arehythmias
Sodium lactate
Least cardiotoxic anti-arrhythmic. DOC for ventricular arehythmias post MI and digoxin induced arrhythmias.
Lidocain - Class 1B antiarrhythmic
Contraindicated for post MI arrhythmias
Flecainide - Class 1C antiarrhythmic. Used for refractory arrhythmias.
Post MI prophylaxis against sudden death, can also be used for thyrotoxicosis
Propanolol - class 2 anti arrhythmic
Usually given for A-fib, hallmark is prolongation of AP duration and increase in QT interval
Class 3 antiarrhythmics
Beta blocker antiarrhythmic that has class 3 properties
Sotalol
A super antoarrhythmic with a SE of microcrystalline deposits in cornea and skin
Amiodarone - Class 3 anti arrhythmic. Used for refractory arrhythmias
Effective in arrhythmias that must traverse calcium dependent cardiac tissue (AV node)
Class 4 antiarrhythmics - PR interval consistently increased
Evoke a compensatory sympathetic discharge which facilitates arrhythmias rather than terminating them
Dihydropyridine CCBs
Miscellaneous antiarrhythmic which is the DOC for paroxysmal SVT
Adenosine
Site of action of carbonic anhydrase inhibitors (Acetazolamide)
Proximal Convoluted Tubule
Why is acetazolamide used in treating mountain sickness
Acetazolamide causes metabolic acidosis resulting to increased respiration
Site of uric acid transport
Proximal convoluted tubule
Site of action of loop diuretics, site of Ca and Mg reabsorption
Thick ascending limb of the loop of henle
Site of action of thiazide diuretics, pumps Na and Cl out of the lumen via the Na/Cl carrier
Distal convoluted tubule
Calcium is reabsorbed in this segment under the control of PTH
Distal convoluted tubule
Site of action of potassium sparing diuretics
Cortical collecting duct
Steroid inhibitors of cytoplasmic aldosterone receptor in CCD. Can cause gynecomastia
Spironolactone - potassium sparing diuretic
Retains water in tubule by reducing reabsorption in proximal tubules, descending limb of the loop of Henle and collecting ducts
Mannitol - osmotic diuretic
Site of action of ADH agonists and antagonists
Medullary collecting duct
Condition that occurs with rapid correction of hyponatremia
Central pontine myelinolysis
Increase number of high affinity LDL receptors which clear LDL and VLDL remnants from the blood
Statins
Reversible competitive inhibitor of HMG COA reductase
Simvastatin - given before bedtime
Binds bile acids, preventing their reabsorption and increasing cholesterol utilization for replacement
Cholestyramine - bile acid binding resin, modestly lowers LDL levels
A transport process in jejunal enterocytes that mediates GI uptake of cholesterol and phytosterols. Inhibited by Ezetimibe
NPC1L1 transporter
Cholesterol analog. Takes the place of dietary and biliary cholesterol, decreasing intestinal absorption
Sitosterol
Most effective agent for increasing HDL levels
Niacin
Pre treatment with this drug reduces Niacin associated flushing
Aspirin
Activates PPAR alpha and increases expression of lipoprotein lipase and apolipoproteins. DOC for hypertriglyceridemia.
Gemfibrozil - lowers triglycerides, increases HDL
Disadvantage of Fibrate + Resin
Increased risk of cholelithiasis
Disadvantage of Statin + Fibrate
Increased risk of myopathy and rhabsomyolysis
Combinations for familial hypercholesterolemia
Niacin + Statin, Statin + Ezetimibe
Histamine is formed from what amino acid?
Histidine
How do you detect an excess production of histamine?
Measurement of Imidazole acetic acid in the urine
Triple response effect of histamine
Wheal, flush and flare
Histamine receptor in stomach, heart and mast cells
H2
Histamine receptor in smooth muscle
H1
Histaminergic agent with anti-motion sickness effect
Meclizine - H1 receptor antagonist (1st generation)
Histaminergic agent that reduces gastric acid secretion
Cimetidine - H2 receptor antagonist
Serotonin is produced from what amino acid?
Tryptophan
How is excess production of serotonin detected?
5-HIAA in urine
Serotonin receptor in the brain
5 - HT 1D
Serotonin receptor in the sensory and enteric nerves
5-HT 3
DOC for acute migraine
Sumatriptan - 5-HT 1D agonist, causes vasoconstriction
DOC for chemotherapy and post-operative vomiting
Ondansetron - 5-HT 3 receptor antagonist
Antidote for ergotamine (5 HT2 receptor antagonist)
Nitroprusside
5 HT2 receptor antagonist that has a SE of retroperitoneal fibrosis
Methysergide
2nd line treatment for migraine and cluster headache
Ergotamine - 5 HT2 receptor antagonist
5 HT2 receptor antagonist with uteroselective effects
Ergonovine (Methylergonovine) - postpartum bleeding
Eicosanoid receptor that acts as a slow reacting substance of anaphylaxis
LTC4, LDT4
Eicosanoid receptor that maintains PDA
PGE1 and PGE2
Eicosanoid receptor for platelet aggregation
TXA2
PGE1 analog that maintains PDA. Can also be used for erectile dysfunction
Alprostadil - vascular smooth muscle relaxation and vasodilation
Prostaglandin I2 analog used for pulmonary HTN
Epoprostenol
Prostaglandin F2 alpha analog used in the treatment of Glaucoma
Latanoprost - can alter color of the eyelid causing permanent eye color change
DOC for acute asthma attacks
Albuterol/Salbutamol - short acting beta 2 selective agonist with a SE of tachycardia
Long acting beta 2 selective agonist used for asthma prophylaxis
Salmeterol
Muscarinic receptor antagonist used for asthma and COPD
Ipratropium - SE of dry mouth
Methylxanthine used as a prophylaxis for asthma nocturnal attacks
Theophylline - SE of seizures, beta blockers can be used as an antidote in overdosage
Mast cell stabilizer used as an asthma prophylaxis and for allergies. No bronchodilator action
Cromolyn
DOC for asthma prophylaxis
Fluticasone - corticosteroid that inhibits phospholipase A2
SE of Fluticasone
Oropharyngeal candidiasis (oral thrush) - gargle after inhaling
Treatment of severe refractory asthma (status asthmaticus)
IV hydrocortisone
Blocks cysteinyl leukotriene 1 receptor for leukotrienes CD4, D4 and E4. Used as asthma prophylaxis
Montelukast - no bronchodilator action
Prophylaxis of severe, refractory asthma not responsive to all other drugs
Omalizumab - anti IgE antibody
Anemia caused by a deficiency of Vit B12 or Folic Acid
Megaloblastic anemia - pernicious anemia most common type
Intrinsic factor is made from?
Parietal cells
Side effect of ferrous sulfate
Black stools - may obscure acute GI loss
Heavy metal chelator used in the treatment of acute iron poisoning and hemachromatosis not adequately treated by phlebotomy
Deferoxamine - chelates excess iron
State of chronic iron overload. Triad?
Hemochromatosis / “Bronze Diabetes” - cirrhosis, DM, skin pigmentation
Neurologic defects in Vit B12 deficiency
Ataxic gait, impaired position and vibratory sense, spasticity
Plasma transport of Vit B12 is accomplished by binding to?
Transcobalamin II
What are the 2 available forms of Vit B12?
Cyanocobalamin and Hydroxocobalamin
Large amounts of Vit B12 is stored in the?
Liver - 5 year supply
Where is folic acid readily absorbed?
Proximal jejunum - modest amounts stored in the body
Performance enhancing drugs in athletes. Production is stimulated by hypoxia
Epoetin Alfa - hematopoietic growth factor . Used for anemia associated with chronic renal failure
Used for neutropenia associated with chemotherapy
G CSF - myeloid growth factor, accelerates neutrophil recovery
For secondary prevention o thrombocytopenia in patients undergoing cytotoxic chemotherapy
Oprelvekin - megakaryocyte growth factor that activates IL 11 receptors
Nonselective, irreversible COX 1 and 2 inhibitor. Reduces platelet production of Thromboxane A2
Aspirin - toxic dose of 150mg/kg, lethal dose of 500mg/kg
What is the triad of aspirin hypersensitivity?
Samter triad - asthma, aspirin sensitivity, nasal polyps
Mechanism of aspirin intoxication that leads to HAGMA
Uncoupling of oxidative phosphorylation
What is the presentation of aspirin intoxication in adults? Children?
Adults - respiratory alkalosis with HAGMA, Children - HAGMA only
Drug that is next in line if the patient has an aspirin allergy
Clopidogrel - irreversibly inhibits binding of ADP to platelet receptors
Antiplatelet drug that interferes with GPIIb/IIIa binding to fibrinogen
Abciximab - used during PCI to prevent thrombosis
Antiplatelet drug that inhibits phosphodiesterase III and increases cAMP, can also cause vasodilation
Dipyridamole - by itself has little or no benefit, contraindicated in heart failure
Drugs use mainly for the prevention and treatment of venous thrombosis
Anticoagulants - inhibit formation of fibrin clots
Heparin vs Warfarin: onset?
Heparin - rapid (minutes), Warfarin - slow (days)
Heparin vs Warfarin: site of action
Heparin - blood, Warfarin - liver
Heparin vs Warfarin: MOA
Heparin - activates antithrombin III, Warfarin - impairs post translational modification of factors X IX VII II (1972)
Heparin vs Warfarin: antidote
Heparin - protamine, Warfarin - vit K or FFP
Heparin vs Warfarin: monitoring
Heparin - PTT, Warfarin - PT
DOC for anticoagulation during pregnancy
Heparin - activates antithrombin III which inactivates thrombin or factor IIa, IXa, Xa by forming stable complexes with them
Anticoagulant that binds and potentiates effect of abtithrombin III on factor Xa (more selective)
Enoxaparin - less risk of thrombocytopenia (vs heparin), does not require monitoring with PTT
Anticoagulation in patients with heparin induced thrombocytopenia
Lepirudin - binds to thrombin’s active site and inhibits its enzymatic action
Anticoagulant that inhibits vit K epoxide reductase, used for chronic anticoagulation
Warfarin - SE of warfarin induced skin necrosis, has a narrow therapeutic window
Thrombolytic drug that has a SE of cerebral hemorrhage
Alteplase (streptokinase) - converts plasminogen to plasmin, degrades the fibrin and fibrinogen
Antidote to Alteplase
Aminocaproic acid (Tranexamic acid) - competitively inhibits plasminogen activation
Causes a severe infusion reaction when administered too fast (dyspnea, chest and back pain)
Vit K - antidote to warfarin, can also prevent hemorrhagic diatheses in newborns
Drug that increases the factor VIII activity of patients with mild Hemophilia A or von Willebrand disease
Desmopressin - vasopressin V2 receptor agonist (ADH agonist)
NSAID and antiplatelet drug that is contraindicated in gout
Aspirin - prevents uric acid excretion
At what doses do aspirin produce anti-inflammatory effects?
High doses (2400-4000 mg/d)
Drug used for post surgical analgesic control. The only IV NSAID, use restricted to 72hrs only
Ketorolac - nonselective reversible COX 1 and 2 inhibitor, inhibits prostaglandin synthesis
NSAID used to close PDA
Indomethacin - nonselective reversible COX 1 and 2 inhibitor, inhibits prostaglandin synthesis
N-acetylcysteine is the antidote for?
Paracetamol - selectively inhibits COX 3, mild analgesic and antipyretic
Cytotoxic intermediate in paracetamol overdose
NAPQI - centrilobar region (zone III) preferentially involved
DMARD of first choice to treat rheumatoid arthritis
Methotrexate - inhibits AICAR transformylase and thymidylate synthetase, may cause a pseudolymphomatous reaction
Drug for Crohn’s disease but may cause reactivation of latent TB
Infliximab - DMARD that binds to TNF alpha
DMARD used to treat RA and IBD but may cause bone marrow suppression, increased risk of infections. Never give with Allopurinol.
Axathioprine - forms 6 Thioguanine, suppressing B and T cell function and immunoglobulin production
DMARD and cancer chemotherapeutic drug that may cause hemorrhagic cystitis. Rescue agent is MESNA
Cyclophosphamide - forms phosphoramide mustard, which cross links DNA to prevent cell replication. Also suppresses T and B cell function
DMARD used during tissue transplantation
Cyclosporine - inhibits IL 1 and 2 receptor and T cell responsiveness
DMARD that may cause reversible myelosuppression
Mycophenolate mofetil - inhibits inosine monophosphate dehydrogenase and T cell lymphocyte proliferation
DMARD that may cause hemolytic anemia, methemoglobinia and reversible infertility in men
Sulfasalazine - sulfapyridine inhibits the release of inflammatory cytokines
MOA of Colchicine
Inhibits microtubule assembly - may cause agranulocytosis, hepatic necrosis
NSAID that is commonly used in the initial treatment of gout as the replacement for Colchicine
Indomethacin - inhibit urate crystal phagocytosis
Uricosuric agent that competes with uric acid for reabsorption in the proximal tubules
Probenecid - may precipitate acute gout during early phase of drug administration (co administer with colchicine)
First line treatment for chronic gout
Allopurinol - alloxanthine irreversibly inhibits xanthine oxidase and lowers production of uric acid
Side effect of Allopurinol
Cataracts
Xanthine oxidase inhibitor used if the patient has an Allopurinol intolerance
Febuxostat