PHARM Flashcards
3 direct cholinergic agonists
Carbachol
Bethanechol
Pilocarpine
6 Cholinergic Antagonists
Atropine Ipratropium Scopolamine Benztropine Oxybutynin Glucopyrrolate
4 Indrect cholinergic agonists (anti-acetylcholinesterases)
Neostigmine
Echothiophate
Donepezil
Edrophonium
Nicotinic antagonist
Hexamethonium
Cholinesterase regenerator
Pralidoxime
a1 a2 b1 b2 agonist
epinephrine
a1 a2 b1 agonist
norepinephrine
D1=D2 > B1 > a1 agonist
Dopamine
B1=B2 agonist
Isoproterenol
B2>B1 agonist
Dobutamine
a1>a2 agonist
Phenylephrine
HIV Rx that cause pancreattis
Ritonavir
NRTIs: Didanosine, stavudine, zalcitabine
HIV Rx that cause rash
NNRTIs: Nevirapine, Delavirdine, Efavirenz
Abacavir
Which HIV Rx cause lactic acidosis
All NNRTIs except abacavir
Which HIV Rx cause peripheral neuropathy?
NRTIs (Didanosine, Stavudine, Zalcitabine)
What birth defect results from lithium?
Ebstein anomaly - displacement of posterior and septal tricuspid valve leaflets towards the apex which leads to atrialization of the right ventricle.
It is associated with Wolff-Parkinson White
Which receptors use a Gs protein? There are 5.
B1, B2, V2, H2, D1
Name 3 drugs that regulate the secretion of gastric acid.
PPIs
H2 blockers
Anti-muscarinics (atropine)
Antacid that may cause diarrhea
Magnesium hydroxide
Antacid that may cause constipation
Aluminum hydroxide
Antacid that may cause rebound hypercalcemia
Calcium carbonate
Electrolyte abnormality commonly seen in administration of antacids
Hypokalemia
Main MOA of prokinetic agents
Increased ACh
Increased 5-HT
Decreased D2
MOA of Metoclopramide
Stimulates 5-HT4
Inhibits D2
Prokinetic agent –increases contractility and tone at rest
Indicated in diabetics with gastroparesis
MOA of Domperidone
Inhibits D2
MOA of Cisapride
Stimulates 5-HT4
5 drugs known to cause seizures
Metoclopramide Buproprion Tramadol Enflurane Evening primrose oil
MOA of protease inhibitors
Inhibit viral assembly by blocking protease enzyme
MOA of fusion inhibitors
Bind viral glycoprotein 41, thus inhibiting fusion iwth CD4 cells
How does aspirin cause Reye syndrome?
The metabolites of aspirin inhibit mitochondrial enzymes, thus decreasing beta oxidation.
Medications used in treatment of chronic hep B and hep c?
IFN alpha is used to treat chronic hep B and hep C.
Ribavirin is also used to treat hep C.
Cocktail of meds taken by patients suffering from severe cirrhosis (4).
Lactulose to treat encephalopathy.
Vitamin K to allow for maximum clotting potential (they are not producing coagulation factors as well –their liver sucks)
Diuretics to treat ascites or edema.
A beta blocker to prevent bleeding from esophageal varices.
MOA of drug of choice in hepatic encephalopathy
LACTULOSE
Lactulose is a sugar that is not absorbed by the enterocytes. So the bacteria metabolize lactulose, creating this acidic environment. NH3 passes by the colon and it gets acidified – > as a cation (NH4+), it can not get back into the body. Thus it is excreted in the stool.
Drug that inhibits conversion of dopa –> dopamine
Carbidopa (it is inhibiting dopa decarboxylase)
Treatment for cystinuria
Acetazolamide – CAI that alkalinizes urine (prevents cystine stones)
Volume of distribution equation
Vd=amount of drug given (IV) / [drug] in plasma
Clearance equation
Cl=0.7 x Vd / T(1/2)
Loading Dose equation
LD = Css x Vd
Maintenance dose equation
MD = Css x Cl
7 P450 inhibitors
PICK EGS Protease inhibitors Isoniazid Cimetidine Ketoconazole Erythromycin Grapefruit juice Sulfonamides
7 P450 inducers
BCG PQRS Barbiturates Carbamazepine Griseofulvin Phenytoin Quinidine Rifampin St. John's Wort
pKa definition
the pH at which the amount of non-protonated form (A- or B) is equal to the amount of protonated form (HA or BH+)
Tx for an acidic drug overdose (e.g. salicylates)
NaHCO3
Traps acidic drug in basic urine
Tx for basic drug OD (e.g. amphetamines)
NH4Cl
Traps basic drug in the acidic urine
General byproduct of Phase I metabolism and 3 reactions that take place
Slightly more polar metabolites
Oxidation, reduction, and hydrolysis
General byproduct of Phase II metabolism and 3 reactions that take place
Very polar metabolites (aka very inactive; thus easily renally excreted)
Acetylation, sulfation, glucuronidation
Which hepatic phase of metabolism is lost first by geriatric patients?
Phase I
Which hepatic phase of metabolism is mediated by CYP450?
Phase I
4 Rx that cause disulfiram like reactions
Metronidazole
Certain cephalosporins
Procarbazine
1st generation sulfonylureas
Rx that inhibits alcohol dehydrogenase
Fomepizole
Rx that inhibits acetaldehyde dehydrogenase
Disulfiram
Ends in -tidine
H2 blockers
Ends in -mustine
Nitrosoureas
Ends in -glitazone
Thiazolinediones
Treatment for heparin-induced thrombocytopenia?
Anti-coagulate! Lepirudin or bivalirudin (direct thrombin inhibitors)
Diabetes drug that causes lactic acidosis (rare but serious)
Metformin
Diabetes drug thats most common SE is hypoglycemia
Sulfonylureas (gliburide, glipizide)
MOA of sulfonylureas
Closes potassium channel on the beta cells causing depolarization. This leads to an influx of calcium, causing insulin release!
MOA of acarbose
Inhibits alpha-glucosidase at intestinal brush border
MOA of pioglitazone (TZDs)
Agonist at PPAR gamma receptors
MOA of heparin
Cofactor for activation of anti-thrombin. Decreasing thrombin and decreasing factor Xa.
MOA and advantages of LMWH
Enoxaparin and dalteparin act more on factor Xa.
Better bioavailability and longer half life.
Can be admin subcutaneously and without lab monitoring.
Rx used in pateitns with HIT
Lepirduin and bivalirudin (direct thrombin inhibitors) that are derivatives of hirudin, the anticoagulant used by leeches.
These are used as an alternative to heparin for anticoagulating patients with HIT.
Drug that increases [Warfarin]
Sulfonamide abx
3 drugs that decrease [Warfarin]
Bile acid sequestrants (e.g. cholestyramine)
St. John’s Wort
Vitamin K
Lab value not altered by warfarin
Bleeding time
Lab values seen in thrombolytic use
Increased PT and PTT
NO CHANGE IN PLATELET COUNT.
MOA of thrombolytics
Directly or indirectly aid conversion of plasminogen to plasmin which cleaves thrombin and fibrin clots.
Toxicity of thrombolytics is treated with
aminocaproic acid
MOA of Hydroxyurea
Inhibits ribonucleotide reductase thus decreasing the production of deoxyribonucleotides.
-indicated for use in sickle cell anemia, CML, psoriasis, myeloproliferative d/o, etc.
MOA of methotrexate
Inhibits eukaryotic dihydrofolate reductase (unlike TMP which inhibits prokaryotic dihydrofolate reductase)
MOA of mycophenolate
A reversible inhibitor of inosine monophosphate dehydrogenase (IMPDH) in purine (guanine) biosynthesis which is necessary for the growth of T cells and B cells
MOA of 6-mercaptopurine
Inhibits purine nucleotide synthesis and metabolism by inhibiting an enzyme called Phosphoribosyl pyrophosphate amidotransferase (PRPP Amidotransferase) – the rate limiting enzyme of purine synthesis. Thus, 6-MP alters the synthesis and function of RNA and DNA. It also interferes with nucleotide interconversion and glycoprotein synthesis.
MOA of linezolid
Binds 50S, blocking translocation
MOA of Rifampin
Inhibits prokaryotic RNA polymerase
HIV rx that causes bone marrow suppression
Zidovudine
Tx for lead poisoning
- In adults?
- In children?
In adults: succimer, EDTA
In kids: dimercaprol, EDTA, succimer
An 11 y.o. child presents with a chronic non-healing ulcer and a small calcified spleen. What drug can improve his sx?
Hydroxyurea
Hint: this is SCD
MOA of streptokinase
Directly or indirectly aid conversion of plasminogen to plasmin which cleaves thrombin and fibrin clots.
MOA of clopidogrel/ticlopidine
Inhibits platelet aggregation by irreversibly blocking ADP receptors. Also inhibits fibrinogen binding by preventing glycoprotein IIb/IIIa from binding to fibrinogen.
MOA of Abciximab/Eptifibatide/Tirofiban
Bind glycoprotein receptor IIb/IIIa on activated platelets, preventing aggregation.
Used in NSTEMIs.
6 hormones that use tyrosine kinase receptors
Insulin IGF-1 FGF PDGF Prolactin Growth hormone
3 drugs that stimulate NE release
Amphetamine
Ephedrine
Tyramine
3 drugs that inhibit NE reuptake
Cocaine
TCAs
Amphetamine
CD4<200 begin prophylaxis with?
TMP-SMX
Dapsone or aerosolized pentamidine
Prophylaxis for PCP
CD4<100 begin prophylaxis with
TMP-SMX
Dapsone pentamidine + leucovorin
Prophylaxis for toxo if there is a + toxo IgG titer
CD4 <50 begin prophylaxis with
Single weekly dose of azithromycin to prevent a MAC infection.
Drug that interferes with Gp120
Miraviroc (CCR5)
Drug that interferes with Gp41
Enfuvirtide
Tx for E. coli infections
TMP-SMX
Fluoroquinolones
3 drugs that cause photosensitivity reactions
SAT for a photo
Sulfonamides
Amiodarone
Tetracyclines
8 drugs to be avoided in patients with an allergy to sulfa
Celecoxib Furosemide Probenecid Thiazides TMP-SMX Sulfasalazine Sulfonylureas Acetazolamide
4 drug (classes) that cause Stevens Johnson syndrome
Penicillins
Sulfa drugs
Seizure drugs
Allopurinol
4 clinical uses of TMP-SMX
UTIs
Shigella/Salmonella
MRSA
AIDS - pneumocystis jiroveci pneumonia CD4<200
MOA and indications for Nitrofurantoin
Bacteriocidal –reduced by bacterial proteins to a reactive intermediate that inactivates bacterial ribosomes.
Indicated for UTI cystitis (not pyelonephritis) by E. coli or S. saprophyticus (not Proteus)
Safe in pregnancy :)
Indications for fluoroquinolones
Gram - (1st and 2nd generation like cipro)
Pseudomonas
Gram + (3rd and 4th generation like levo and moxi, respectively)
1 time you can use fluoroquinolones in pediatric patients
Cystic fibrosis
6 bugs treated with Metronidazole
GET GAP on the Metro Giardia lamblia Entamoeba histolytica Trichomonas Gardnerella vaginalis Anaerobes H. pylori
Tx for Chaga’s disease
Nifurtimox
4 treatments for resistant malarias
Quinine + doxycycline
Mefloquine
Atovaquone-proguanil
Artemether-lumefantrine
Tx for cutaneous leishmaniasis
Sodium stibogluconate
Tx for visceral leishmaniasis
Liposomal ampho B
How does the body metabolize 6-mercaptopurine?
Xanthine oxidase
Thus toxicity is increased if used with allopurinol (would use 6-thioguanine instead)
Anti-cancer drug used in rheumatoid diseases as well as ectopic pregnancies
Methotrexate
For which cancers is dactinomycin particularly useful and what is its MOA?
Wilm’s tumor
Ewing’s sarcoma
Rhabdomyosarcoma
Intercalates in DNA therefore DNA cannot replicate
5 drugs that inhibit microtubules
Vinca drugs (vincristine/vinblastine) Taxanes (paclitaxel) Anti-helminthics (-bendazoles) Griseofulvin Colchicine
Myelosuppression induced by MTX can be reversed with administration of?
Leucovorin –folinic acid “rescue” agent
5-fluorouracil can be used topically to treat?
Actinic keratosis (prevent it from progressing to malignancy)
MOA of Cytarabine
Pyrimidine analog that inhibits DNA polymerase
Drug that chelates iron to prevent cardiotoxicity induced by doxorubicin
Dexrazoxane
2 cancer drugs associated with pulmonary fibrosis
Bleomycin
Busulfan
This alkylating agent is associated with CNS toxicity
Nitrosoureas (the -mustines) cross blood brain barrier and can cause CNS toxicity like dizziness and ataxia.
They are used to treat brain tumors including GBM.
The hemorrhagic cystitis associated with cyclophosphamide can be prevented with what Rx?
Mesna
Binds acrolein which is a toxic metabolite
Toxicity of vincristine
Neurotoxicity (areflexia, peripheral neuritis), paralytic ileus
Toxicity of vinblastine
Vinblastine BLASTS bone marrow (suppression)
3 drugs used to treat testicular cancer
Eradicate Ball Cancer
Etoposide
Bleomycin
Cisplatin
Monoclonal ab against CD20
Rituximab – treats NHL and rheumatoid arthritis
2 anti-cancer agents that cause cardiotoxicity
Doxorubicin – DILATED CARDIOMYOPATHY
Trastuzumab
Toxicity of cisplatin/carboplatin
Acoustic nerve damage and nephrotoxicity
3 anti-cancer agents that cause myelosuppression
5-FU
6-MP
Methotrexate
Antibody against philadelphia chromosome
Imatinib
Intercalates DNA and produces oxygen free radicals
Doxorubicin
Daunorubicin
3 drugs that cause free-radical induced DNA strand breakage
Bleomycin
Doxorubicin
Daunorubicin
Tx for AML
Cytarabine
Tx for CML
Busulfan
Imatinib
Tx for Trypanosoma
Suramin or melarsoprol
When treating a patient long-term with Dapsone (maybe the patient has leprosy or dermatitis herpetiformis from Celiac disease), what would you want to supplement their tx with in order to prevent methemoglobinemia from occurring?
Cimetidine
Treatment for methemoglobinemia
Methylene blue, vitamin C
4 treatment options available for pulmonary hypertension
Bosentan, ambrisentan
Prostaglandin analog (these decrease bronchial tone)
Sildenafil
Dihydropyridine CCB such as nifedipine
MOA of Bosentan
Tx for pulmonary hypertension
Antagonist of endothelium-1 receptor, thus decreasing pulmonary vascular resistance
Name 6 conditions treated with hyperbaric oxygen therapy.
Gas gangrene Decompression sickness Arterial gas embolism CO poisoning Osteomyelitis MI
Tx of choice for toxoplasma gondii
Sulfadiazine + pyrimethamine
Use and MOA of cyproheptadine
1st gen anti-histamine (H1)
Used as appetite stimulant since it has additional anti-cholinergic, anti-serotinergic, and local anesthetic properties
Use and MOA of promethazine
1st gen anti-histamine (H1) with anti-emetic and anti-cholinergic properties
Therefore it is used to tx N/V
Use and MOA of chlorpheniramine
1st gen anti-histamine (H1) used in tx of allergies
Its in several OTC allergy/cold medicines.
Use and MOA of hydroxyzine
1st gen anti-histamine (H1)
Sedative, anti-itch
Use and MOA of meclizine
1st gen Anti-histamine (H1) and anti-emetic
Tx of vertigo
Long-acting prophylactic agents for asthma that may cause tremor and arrythmia
Salmeterol and formoterol (B2 agonists)
MOA of last-resort asthma treatment that blocks the actions of adenosine
Theophylline likely causes bronchodilation by inhibiting phosphodiesterase, thereby decreasing cAMP hydrolysis. Its limited in use due to its narrow therapeutic index, often causing cardiotoxicity and neurotoxicity.
Overdose of theophylline is treated with?
Beta blockers
MOA and use of cromolyn sodium
Inhibits the release of mast cell mediators such as histamine.
Prophylaxis in asthma patients.
MOA of ipratropium, tiotropium
Competitively blocks muscarinic receptors, preventing bronchoconstriction. Used in asthma and COPD.
1st line inhaled therapy for chronic asthma and MOA
Corticosteroids – Beclomethasone and fluticasone
These inhibit the synthesis of virtually all cytokines. They inactivate NF-kB, the transcription factor that induces the production of TNF alpha among other inflammatory agents.
Tx for aspirin-induced asthma and MOA
Montelukast (better in 1 y.o. and up)
Zafirlukast (5 y.o. and up)
Block leukotriene receptors – think lu kast = “last” ste in leukotriene synthesis
MOA of zileuton
5-lipoxygenase pathway inhibitor that blocks the conversion of arachidonic acid to leukotrienes
Drug used for allergic asthma resistant to inhaled steroids and long-acting B2 agonists and its MOA
Omalizumab –monoclonal anti-IgE Ab that binds mostly unbound serum IgE
What 3 conditions can be treated with N-acetylcysteine?
CF –cleaves disulfide bonds within mucous glycoproteins, thus loosening mucus plugs.
Antidote in acetaminophen OD as it regenerates glutathione (an anti-oxidant).
Can be taken orally to protect kidneys against contrast-induced nephropathy, as in diabetics with renal failure who need an emergency contrast CT.
3 things you need to check before placing a patient on amiodarone
Liver function tests
Pulmonary function tests
Thyroid function tests
2 major treatments of choice in anaerobic infections
Metronidazole
Clindamycin
Clinical uses for ampicillin/amoxicillin
H. influenzae E. coli, enterococci Listeria Proteus mirabilis Salmonella, Shigella
Hint: HEELPSS
3 anti-pseudomonal penicillins
Ticarcillin
Carbencillin
Piperacillin
Two different mechanisms of resistance used against penicillin agents
B-lactamase
Alteration of PBPs
2 beta lactamase inhibitors
Sulbactam
Clavulanic acid
Name 4 penicillinase-resistant penicillins and their toxicity.
Oxacillin, nafcillin, dicloxacillin, methicillin
Can cause interstitial nephritis
Drug that increases the half life of Penicillin G via blocking active renal secretion of penicillin
Probenicid
Jarish-Herxheimer phenomenon
Acute worsening of sx (fever, HA, muscle pains) soon after Pen G treatment due to released pyrogens from killed organisms, especially with tx of Syphilis
2 first gen cephalosporins and their clinical use.
Cefazolin, cephalexin PEcK Gram + cocci Proteus mirabilis E. coli Klebsiella pneumonia
3 second gen cephalosporins and their clinical uses
Cefoxitin, cefaclor, cefuroxime Gram + cocci, HEN PEcK** H. influenzae Enterbacter Neisseria Proteus mirabilis E. coli Klebsiella pneumonia Serratia marcescens
3 third gen cephalosporins and clinical uses.
Ceftriaxone, cefotaxime, ceftazidime
Serious gram negative infections resistant to other B lactams.
Ceftriaxone: Meningitis, CAP, gonorrhea
Ceftazidime: P. aeruginosa
4th generation cephalosporin and clinical use
Cefepime
Super broad spec. Increased activity against Pseudomonas and gram + organisms.