Pharmacology Flashcards
Alpha-1
Gq
* Vascular smooth muscle, pupillary dilator contraction, intestinal and bladder sphincter contraction
Alpha-2
Gi
* Decrease insulin, lipolysis, sympathetic outflow, increase platelet aggregation
Beta-1
Gs
* HR, contractility, renin, lipolysis
Beta-2
Gs
* Vasodilation, bronchodilation, increased HR, contractility, lipolysis, insulin; decreased uterus tone, increased aq. humor, ciliary muscle relaxation
M1
Gq
* CNS, enteric
M2
Gi
* HR/atria
M3
Gq
* Exocrine, miosis, accommodation (ciliary muscle contraction)
D1
Gs
* Relaxes renal vascular smooth muscle
D2
Gi
* Modulate transmitter release (brain)
H1
Gq
* Nasal and bronchial mucus production, contraction bronchioles, pruritis, pain
H2
Gs
* Gastric acid
V1
Gq
* Vascular smooth muscle contraction
V2
Gs
* Collecting tubules (2 kidneys)
- Match
DAG/PKC
IP3/Ca
DAG = PKC IP3 = Ca2+
Protein kinase A –>
Myosin light chain kinase (smooth muscle)
MOA Amphetamine
Releases stored catecholamines
Indirect sympathomimetics (3)
- Amphetamine
- Ephedrine
- Cocaine
MOA Ephedrine
Releases stored catecholamines
Uses Amphetamine
Narcolepsy, obesity, ADHD
Uses Ephedrine
Nasal decongestion, urinary incontinence, hypotension
MOA Cocaine
Reuptake inhibitor
Uses cocaine
Vasoconstriction/local anesthesia
You should never give beta-blockers with cocaine intoxication because…
Can lead to unopposed alpha-1 activation and extreme hypertension
Antidote to acetaminophen toxicity
N-acetylcysteine (replenishes glutathione)
Antidote to salcylates toxicity
NaHCO3 (alkalinize urine), dialysis
Antidote to amphetamine toxicity
Nh4Cl (acidify the urine)
Antidote to AchE inhibitor (OP) toxicity
Atropine, pralidoxime
Antidote to anti-muscarinic toxicity
Physostigmine salicylate, control hyperthermia
Antidote to beta-blocker toxicity
Glucagon
Antidote to digitalis toxicity
KLAM
- Normalize K
- Lidocaine
- Anti-dig Fab
- Mg2+
Antidote to Fe toxicity
Deferoxamine, deferasirox
Antidote to lead poisioning
EDTA, dimercaprol, succimer, penicillamine
Antidote to mercury, arsenic, gold
Dimercaprol, succimer
Antidote to Cu, arsenic, gold
Penicillamine
Antidote to CN toxicity
Nitrate + thiosulfate; hydroxocobalamin
Antidote to Methemeglobin
Methylene blue, vitamin C
Antidote to CO toxicity
O2
Antidote to methanol, ethylene glycol toxicity
Fomepizole > ETOH, dialysis (alcohol DH)
Antidote to opioid toxicity
Naloxone, Naltrexone
Antidote to benzo toxicity
Flumazenil
Antidote to TCA toxicity
NaHCO2 (plasma alk)
Antidote to heparin toxicity
Protamine
Antidote to warfarin toxicity
Vitamin K, FFP
Antidote to TPA/streptokinase/urokinase toxicity
Aminocaproic acid
Antidote to theophylline toxicity
Beta-blocker
Sulfa drugs
Popular FACTSSS
Probenecid, Furosemide, Acetazolamide, Celecoxib, Thiazide, Sulfonamide, Sulfasalazine, Sulfonurea
Patients with sulfa allergy may develop…
Fever, UTI, pruritic rash, SJ, hemolytic anemia, TBO, agranulocytosis, hives
P450 Inducers
APPCR (Chronic ETOH, phenytoin, phenobarbital, carbamazepine, rifampin)
Modafinil
St. John’s Wort
Griseofulvin
P450 Inhibitors
MAGIC RACKS GQ
Macrolides, Amiodarone, Grapefruit juice, INH, Cimetidine, Ritonavir, acute ETOH, Cipro, Azoles, Sulfonamides, Gemfibrozil, Quinidine
ADR: Coronary vasospasm (3)
Cocaine, sumatriptan, ergot alkaloids
ADR: Cutaneous flushing (4)
VANC
Vancomycine, Adenosine, Niacin, CCB
ADR: Dilated cardiomyopathy (2)
Doxorubicin (Adriamycin), Daunorubicin
ADR: TDP (2)
Class IA: Quinidine
Class 3: Sotalol
ADR: Agranulocytosis (6)
Clozapine, Carbamazepine, Colchicine, Dapsone, PTU, Methimazole
ADR: Aplastic anemia (5)
Chloramphenicol, benzene, NSAIDS, PTU, Methimazole
ADR: AIHA (Direct Coombs positive)
Methyldopa, penicillin
ADR: Gray baby syndrome (1)
Chloramphenicol
ADR: Hemolysis in G6PD patients (5)
IS PAIN
INH, Sulfonamides, Primaquine, ASA, Ibuprofen, Nitrofurantoin
ADR: Megaloblastic anemia (3)
Phenytoin, MTX, Sulfa drugs
ADR: Thrombotic complications
OCP’s (estrogens)
ADR: Cough
ACE inhibitors (not ARB’s)
ADR: Pulmonary fibrosis (3)
Amiodarone, Bleomycin, Busulfan
ADR: Acute cholestatic hepatitis, jaundice (1)
Erythromycin
ADR: Focal to massive hepatic necrosis (4)
HAVAc
Halothane, Amantia phalloides, Valproate, Acetaminophen
ADR: Hepatitis
INH
ADR: C. diff (2)
Clindamycin, ampicillin
ADR: Adrenocortical insufficiency (1)
GC withdrawal
ADR: Gynecomastia (6)
Some Drugs Create Awkward Knockers
Spironolactone, Digitalis, Cimetidine, ETOH (chronic), Estrogens, Ketoconazole
ADR: Hot flashes (2)
Tamoxifen, clomiphene
ADR: Hyperglycemia (5)
Niacin, Tacrolimus, Protease inhibitor, HCTZ, CS
ADR: Hypothyroidism (3)
Lithium, amiodarone, sulfonamides
ADR: Fat redistribution (2)
PI, GC
ADR: Gingival hyperplasia (2)
Phenytoin, Verapamil
ADR: Gout
Furosemide, Thiazides, Niacin, Cyclosporin
ADR: Osteoporosis
Heparin, CS
ADR: Anti-muscarinic (4)
Atropine, TCA, H1 blocker, neuroleptics
ADR: Disulfram-like reaction
Metronidazole, CS, Procarbazine, 1st generation sulfonureas
ADR: Nephro/ototoxicity
AG, Vanco, Loop diurectics, cisplatin
ADR: Tardive dyskinesia
Antipsychotics
ADR: Seizures
I BITE My tongue
INH, Bupropion, Imipenim/cilastatin, Tramadol, Enflurane, Metoclopramide
ADR: Parkinson’s
Antipsychotics, reserpine, metoclopramide
ADR: Cinconism
Quinidine, quinine
ADR: SIADH
Carbamazepine, Cyclophosphamide
ADR: I/S nephritis
Methicillin, NSAIDS, Ferosemide
ADR: Hemorrhagic cystitis
Cyclo/Ifosfamide (mesna)
ADR: Fanconi’s syndrome
Expired tetracycline
ADR: DI
Lithium, democlocycline
ADR: Tendonitis, tendon rupture, cartilage damage
FQ’s
ADR: Teeth kids
Tetracyclines
ADR: SLE-like syndrome
HIPP
Hydralazine, INH, Procainamide, Phenytoin
ADR: Myopathy
Fibrates, Niacin, Colchicine, Hydroxychloroquine, IFN-alpha, Penicillamine, Statins, GC
ADR: Osteoporosis (2)
CS, heparin
ADR: Photosensitivity (3)
Sulfonamides, Tetracycline, Amiodarone
ADR: SJ/Rash
PEC SLAPP
Penicillin, Ethosuximide, Carbamazepine, Sulfa, Lamotrigine, Allopurinol, Phenytoin, Phenobarbital
Platelet aggregation inhibitors (4 classes)
- COX inhibitors: ASA
- PDE inhibitors: Dipyramidole, Cilastazol
- ADP R blockers: Clopidogrel, Ticlopidine,
- Gp2b/3a blockers: Abciximab, Eptifibratide, Tirofiban
ADP receptor blockers (4)
Clopidogrel, Ticlopidine, Ticagrelor, Prasugrel
Clopidogral and Omeprazole interaction
Omeprazole inhibits CYP and clopidogrel requires CPY2C19 to be activated
Four classes of anti-coagulants
- Indirect thrombin (UFH) & 10 ( LMWH = Fondaparinaux, Enoxaparin/Dalteparin/Tiazaparin)
- DTI (Lepirudin, Bivalirudin, Argatroban PO = dabigatrin etexilate)
- D10I (Rivaroxiban, Apixiban)
- Courmarin (Warfarin)
Thrombolytics
SK, UK, Alteplase, Reteplase, Tenecleplase
Chemical antagonist of heparin
Protamine sulfate
TPAi drug
Aminocaproic acid
Describe HIT
Heparin complexes with platelet factor 4; anti-IgG Ab attack and deposit on platelets; more Factor 4 released.
d/c heparin; DTI/Fondaparinaux & protamine sulfate
Part of nephron: CAI
Uses
AE’s
PCT: Acetazolamide
Use: metabolic alkalosis, mountain sickness, glaucoma, pseudotumor cerebri
AE: metabolic acidosis
Drug used in treatment of pseudotumor cerebri
Acetazolamide
Mannitol contraindications
Anuria, CHF; pulmonary edema/dehydration = AE
Mannitol uses
Drug overdose, elevated ICP/IOP
Loop diuretic that can be used in a patient with sulfa allergy
Ethacrynic acid
AE Furosemide
Ototoxicity, hypokalemia, dehydration, sulfa, IS nephritis, gout
Which diuretic stimulates PGE release and is inhibited by NSAIDS?
Furosemide
MOA HCTZ
NaCl channel in DCT
List 3 thiazide diuretics
- HCTZ
- Chlorthalidone
- Metalozone
Indicated for treatment of Liddle’s syndrome
Triamtrene, Amiloride
Drugs associated with tubulointerstitial nephritis
Sulfonamides (thiazide diurectice), methicillin, cipro, cephalosporins, allopurinol, PPI, rifampin, cimetidine, NSAIDS
What should you think of when the urine dipstick reveals large blood, but the UA shows no RBC’s on microscopy
Rhabdomyolisis (statin)
Which antibiotics are most associated with acute renal failure when combined with cephalosporins?
Aminoglycosides
Which HIV protease inhibitor is associated with crystal induced nephropathy?
Indinavir
In patients with impaired renal function, the loading dose should be the same/higher/lower and the maintenance dose should be the same/higher/lower
LD: same
MD: lower
The 7 classes of anti-hypertensives.
- ACEi/ARB
- Beta blocker
- CCB
- Diuretics
- Alpha antagonists
- Alpha-2 agonists
- Vasodilators
The 3 major classes of angiotensin drugs used to treat HTN
- ACEi (-opril)
- ARB (-artan)
- Renin inhibitors: aliskiren
Aliskiren
Renin inhibitor
The 2 major CI for the use of ACEi’s
- Bilateral renal artery stenosis
2. Pregnancy
Some of the major AE of ACEi’s
- Angioedema
- Cough
- Hyperkalemia
The 2 major classes of calcium channel blockers
- Dihydropyrmidines: Amlodipine, Nifidepine
2. Non-dihydropyrimidines: Verapamil, Diltiazem
Among the CCB’s, which class of drugs is much more selective for the blood vessels vs the heart?
The Dihydropyrmidines (Amlodipine and Nifedipine)
The major AE of Verapamil & its major contraindication
AE: constipation
CI: CHF (2/2 negative inotropic)
The two types of anti-hypertensive treatments useful in black and elderly patients
- Thiazides
2. CCB’s
The preferred beta-blocker in pregnancy
Pindolol
Non-selective beta blockers vs. selective beta blockers
Non-selective: Propranol, pindolol
Selective: Atenolol, metopropol
Should beta-blockers be tapered gradually?
Yes
Beta-blockers are contraindicated in patients with…
COPD and asthmatics
When would it be appropriate to use an alpha-1 blocker to treat a patient with HTN?
If the patient also has BPH
Major AE of alpha-1 blockers? What can be given to prevent this AE?
Reflex tachycardia; give beta-blocker
A mixed alpha-beta blocker example
Labetalol
Labetalol MOA
Mixed alpha-beta blocker
Which alpha-2 agnoist is associated with a positive Coombs test: hemolytic anemia, hepatitis, drug fever?
Methyldopa
Among anti-hypertensive drugs, which one is associated with anti-histone antibodies?
Hydralizine
Which direct vasodilator can be used for the PO treatment of malignant hypertension and can be used topically to treat male pattern baldness?
Minoxidil
What drugs can be used to treat pulmonary hypertension?
PGE (epoprostenol)
Inhibitors of endothelin synthesis (bosentan)
Which pharmacologic treatment of pulmonary hypertension is pregnancy category X?
Bosentan (endothelin receptor blocker)
First line treatment for HTN in pregnancy (along with methyldopa)
Hydralazine
Hydralazine is often administered with a ________________ to prevent this adverse effect
Beta-blocker; reflex tachycardia
MOA Hydralazine
Increases cGMP vasodilates arterioles>veins
2 of the most popular treatments of malignant hypertension
- Nitroprusside
2. Fenoldopam: D1 agonist; decreases BP and increases natriuresis
Drug of choice for patients with catecholamine-related emergencies
Phentolamine
Often used for aortic dissection or postoperative hypertension
Esmolol
Drug of choice in treating hypertensive emergencies in pregnancy related to eclampsia
Hydralazine
Famous AE of sodium nitroprusside
CN toxicity (adminster sodium thiocyanate)
Can CCB’s be used for Prinzmetal’s angina and Raynaud’s phenomenon?
Yes
Are beta-blockers contraindicated in cardiogenic shock?
Yes
Arteries, veins, both: hydralazine, nitrates, ACEi
A: Hydralazine
V: Nitrates
Both: ACEi
What are 2 reasons patients with advanced heart disease have elevated levels of aldosterone?
- Angiotensin stimulation
2. Reduced hepatic clearance
Mild digoxin toxicity is treated with…
Severe toxicity…
Mg, Lidocaine, adjust K to high normal
Severe: pacer, digitalis Ab
Inotrope/Chronotrope: Digoxin
Positive inotrope
Negative chrontrope
HR: nitrates vs. B-blockers/CCB
Nitrates: reflex increase
BB/CCB: decrease
Arterial pressure nitrates vs. B-blockers/CCB
Nitrates: decrease
BB/CCB: decrease
EDV nitrates vs. B-blockers/CCB
Nitrates: decrease
BB/CCB: increase
Contractility nitrates vs. B-blockers/CCB
Nitrates: reflex increase
BB/CCB: decrease
Ejection time nitrates vs. B-blockers/CCB
Nitrates: decrease
BB/CCB: increase
First line treatment of angina
Nitroglycerin
Treatment of unstable angina; 2nd line; 3rd line
NG + beta-blocker
2nd line: CCB; 3rd line Ranolazine
Beta blockers used in the treatment of variant angina?
No
Acute treatment of ventricular arrhythmias from
myocardial infarction or cardiac manipulation
Lidocaine (Class 1B)
Class 1A anti-arrhythmics
Quinidine, Procainamide, Disopyramide
* Intermediate association/dissociation, non-specific K+ channel blockade
Class 1B anti-arrhythmics
Lidocaine, Mexiletine; fast association/dissociation; do not directly block K+ channels
Class 1C anti-arrhythmics
Flecainide, Propafenone; slow association/dissociation; do not directly block K+ channels
Hyper or hypokalemia can increase toxicity for all class 1 anti-arrhythmics
Hyperkalemia
AE Class IA anti-arrhythmics
Diso: heart failure
Quin: cinchonism
Procainamide: SLE
AE Amiodarone
Pulmonary fibrosis, hypothyroidism
Peaked T waves and prolonged PR intervals (which electrolyte disturbance?)
Hyperkalemia
Which anti-arrhythimics are associated with TDP?
Class IA & 3
Drug useful in acute ventricular arrhythmia (post MI) and in digitalis-induced arrhythmias
Lidocaine
Increase, Decrease, No Change in AP duration
Class IA, IB, IC anti-arrhythmics
1A: Increase
1B: Decrease
1C: No change
Which anti-arrhythmics work by decreasing the slope of phase 4?
Class 2 (beta-blockers)
Lipid lowering agents: lower LDL
Statin
Lipid lowering agents: increase HDL
Niacin
Lipid lowering agents: lower TG
Fibrates
Lipid lowering agents: can paradoxically increase TG
Resins
AE: statins
Hepatotoxicity, rhabdomyolysis
Lipid lowering agents: can cause cholesterol gallstones
Fibrates, Resin
Lipid lowering agents: can cause hepatotoxicity
Statin, Fibrate, Ezetimbe
Lipid lowering agents: Can cause red, flushed face, hyperglycemia, acanthosis nigricans, gout
Niacin
Lipid lowering agents: Best for pregnant women and children
Resins
Lipid lowering agents: inhibit conversion of HMG coA to mevalonte
Statin
Lipid lowering agents: inhibits lipolysis in adipose tissue; reduced VLDL secretion
Niacin
Lipid lowering agents: upregulates LPL which increases TG clearance
Fibrates
Lipid lowering agnets: decreases HSL vs. upregulates LPL
Niacin; fibrates
Aldesleukin
IL-2: RCC, metastatic melanoma
Filgrastim vs. Sargramostim
G-CSF
GM-CSF
Alpha-interferon
HBV, HCV, KS, Leukemia, Malignant melanoma
Beta-interferon
MS
Gamma-interferon
CGD
Oprelvekin
IL-11 (TBOcytopenia)
Il-11
TBOpenia (Oprelvekin)
TNF-alpha agents
Infliximab, Adalimumab
Infliximab
TNF-alpha
Adalimumab
TNF-alpha
Trastuzumb
Herceptin (HER2 overexpressing breast cancer)
Rituximab
CD20
Omalizumab
IgE: Additional line treatment for severe asthma
Muromonab-CD3 (OKT3)
CD3 target (prevent acute rejection)
What agent can be used to treat sickle cell anemia? What is its effect? AE?
Hydroxyurea; increases HbF
* AE = cutaneous vasculitis
3 drugs which can deplete folate
- MTX
- Trimethoprim
- Pyrimethamine
2 reactions requiring B12
- Methylmalonyl coA –> succs CoA
2. Homocysteine –> methionine
Anti-CD20-Ab
Rituximab
Rituximab
Anti-CD20-Ab
Cituximab
Anti-EGFR-Ab
Anti-EGFR-Ab
Cituximab
CNI (2)
Cyclosporine, Tacrolimus
mTOR inhibitor
Sirolimus
IL-2 receptor antagonists
Basiliximab, Daclizumab
Anti-TNF-alpha agents
Adalimumab, Etanercept, Infliximab
Stimulates IL-2 (can be used for RCC)
Aldesleukin
Anti-CD3-Ab
Muromonab
First line treatment in multiple myeloma
Thalidomide
Thalidomide MOA
Decreases TNF-alpha production; anti-androgenic
Nitroglycerin increases/decreases myocardial O2 consumption; whereas dobutamine does the opposite
NG: decreases
Dobutamine: increases
Major toxicity: Cyclophosphamide & Ifosfamide
Hemorrhagic cystitis
Major toxicity: Bleomycin
Pulmonary fibrosis
Major toxicity: Cisplatin
Nephrotoxicity & deafness
Major toxicity: Doxorubicin & Daunorubicin
Dilated cardiomyopathy
Major toxicity: Vincristine
Peripheral neuropathy
Major toxicity: Etoposide, MTX and Vinblastine
BM suppression
Major toxicity: L-Asparaginase
Pancreatitis & bleeding
Prevention of Hemorrhagic cystitis by cyclophosphamide & ifosfamide
MESNA
Prevention of Cisplatin induced nephrotoxicity
Good hydration & amifostine
Prevention of Doxorubicin & daunorubicin induced dilated cardiomyopathy
Dexrzoxane
Prevention of BM suppression by CTX agents
Filgrastim
Prevention of MTX induced BM supression
Leucovorin (THF)
Major toxicity: Trastuzumab
Cardiotoxicity
Cell cycle specific CTX agents: G1, S, G2, M
G1: Topo 2 (Etoposide)
S: Anti-metabolites
G2: Bleomycin
M: Vinca & taxanes (MT)
Non cell cycle specific CTX agents
ABX (minus bleomycin), Alkylators, Topo 1 (Camptothecins)
Differentiate between adjuvant and neo-adjuvant CTX
Adjuvant: post SX/Radiation
Neo-adjuvant: pre-surgery
Hydroxyurea affects what stage of the cell cycle?
S phase
The major alkylating CTX agents:
- N mustards (Cyclophosphamide)
- Busulfan - PF, hyperpig
- Carmustine - CNS tumor
- Platinum compounds (cisplatin)
- Dacarbazine, procarbazine
The toxic compound of cyclophosphamide once it is activated by the liver
Acrolein
All TNF-alpha inhibitors predispose to…
Infection, including re-activation of latent TB since TNF blockade prevents activation of macrophages and destruction of phagocytosed microbes
Dronates, i.e. Aldendronate MOA
Pyrophosphate analogs; bind hydroxyapatite in the bone; inhibits osteoclastic activity
Dronates, i.e. Aldendronate use
Osteoporosis, hypercalcemia, Paget’s disease
Dronates, i.e. Aldendronate AE
Osteonecrosis of the jaw; corrosive esophagitis
Dose of 6-MP or Azathioprine must be reduced if co-administered with…
Allopurinol
Myelosupression of MTX is reversible with
Leucovorin
5-FU inhibits
Thymidylate synthase
Supplementing leucovorin with ________ leads to a stronger CTX effect, yet stronger cytotoxic effects
5-FU
AE 5-FU
Skin exfoliation on palm and feet (hand-foot syndrome), photosensitivity
Use Gemcitabine
Pancreatic cancer
ara-C CTX MOA
Competitively inhibits DNA polymerase
Differentiate between the vinca alkaloids and the taxanes MOA
Both are microtubule inhibitors working on M phase; Vinca = prevent MT polymerization; Taxanes = hyperstabalize polymerized MT’s
AE Vincristine
Neuropathy; bone marrow sparing
The 2 bone marrow sparing CTX agents
Vincristine and bleomycin
AE taxanes
Skin toxicity, fluid retention
CTX agent: topoisomerase 2 inhibition
Etoposide and Tenoposide
CTX agent: topoisomerase 1 inhibition
Camptothecin: topotecan, irinotecan
MOA anti-tumor antibiotics
Free radical mediated DNA strand breaks
Radiation recall reaction
Anthracyclines: Doxo/Daunorubicin, Dactinomycin
Dactinomycin is primarily used for…
Childhood tumors
Glaucoma drugs that decrease synthesis of aq humor
Alpha Agonist: Epi, Brimonidine
Beta blocker: timolol, betaxolol, carteolol
Acetazolamide
Glaucoma drugs that increase aq humor outflow
Direct M: Pilocarpine, carbachol
Indirect M: Physostigmine, echothiophate
PGE2-alpha: Latanoprost
Opioid used for cough supression
Dextromethorphan
Opioid used for diarrhea (2)
Lopiramide, Diphenoxylate
Opioid receptors: mu, delta, kappa
Mu: morphine
Delta: Enkephalin
Kappa: dynorphin
Partial mu agonist and kappa agonist that can precipitate pain if used with a full Ag
Butorphanol
Weak opioid gnoist; inhibits serotonin and NE reuptake; used for chronic pain. What is the AE?
Tramadol; increased risk for seizures