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387 Cards in this Set

  • Front
  • Back
Time it takes for amount of drug to fall to half of its value, constant in first order kinetics (majority of drugs)
Half-life (T1/2)
Relates the amount of drug in the body to the plasma concentration
Volume of distribution (VD)
Plasma concentration of a drug at a given time
Cp
The ratio of the rate of elimination of a drug to its plasma concentration
Clearance (CL)
The elimination of drug that occurs before it reaches the systemic circulation
First pass effect
The fraction of administered dose of a drug that reaches systemic circulation
Bioavailability (F)
When the rate of drug input equals the rate of drug elimination
Steady state
This step of metabolism makes drug more hydrophilic and hence augments elimination
Phase I
Different steps of Phase I
Oxidation, reduction, hydrolysis
Products of Phase II conjugation
Glucuronate, acetic acid, and glutathione sulfate
Inducers of Cytochrome P450
Barbiturates, phenytoin, carbamazepine, and rifampin
Inhibitors of CYP450
Cimetidine, ketoconazole, erythromycin, isoniazid and grapefruit
Constant percentage of substrate metabolized per unit time
First order kinetics
Drug elimination with a constant amount metabolized regardless of drug concentration
Zero order kinetics
Target plasma concentration multiplied by (volume of distribution divided by bioavailability)
Loading dose (Cp*(Vd/F))
Concentration in the plasma multiplied by (clearance divided by bioavailability)
Maintenance dose (Cp*(CL/F))
Strength of interaction between drug and its receptor
Affinity
Selectivity of a drug for its receptor
Specificity
Amount of drug necessary to elicit a biologic effect
Potency
Ability of drug to produce a biologic effect
Efficacy
Ability of a drug to produce 100% of the maximum response regardless of the potency
Full agonist
Ability to produce less than 100% of the response
Partial agonist
Ability to bind reversibly to the same site as the drug and without activating the effector system
Competitive antagonist
Ability to bind to either the same or different site as the drug
Noncompetitive antagonist
Mechanism of action (MOA) utilizes intracellular receptors
Thyroid and steroid hormones
MOA utilizes transmembrane receptors
Insulin
MOA utilizes ligand gated ion channels
Benzodiazepines and calcium channel blockers
Median effective dose required for an effect in 50% of the population
ED50
Median toxic dose required for a toxic effect in 50% of the population
TD50
Dose which is lethal to 50% of the population
LD50
Window between therapeutic effect and toxic effect
Therapeutic index
Drug with a high margin of safety
High therapeutic index
Drug with a narrow margin of safety
Low therapeutic index
Antidote used for lead poisoning
Dimercaprol, EDTA
Antidote used for cyanide poisoning
Nitrites
Antidote used for anticholinergic poisoning
Physostigmine
Antidote used for organophosphate and anticholinesterase poisoning
Atropine, pralidoxime
Antidote used for iron salt toxicity
Deferoxamine
Antidote used for acetaminophen (APAP) toxicity
N-acetylcysteine
Antidote for arsenic, mercury, lead, and gold poisoning
Dimercaprol
Antidote used in poisonings: copper (Wilson's disease), lead, mercury, and arsenic
Penicillamine
Antidote used for heparin overdose
Protamine
Antidote used for warfarin toxicity
Vitamin K and Fresh frozen plasma
Antidote for tissue plasminogen activator (t-PA), streptokinase
Aminocaproic acid
Antidote used for methanol and ethylene glycol
Ethanol
Antidote used for opioid toxicity
Naloxone (IV), naltrexone (PO)
Antidote used for benzodiazepine toxicity
Flumazenil
Antidote used for tricyclic antidepressants (TCA)
Sodium bicarbonate
Antidote used for carbon monoxide poisoning
100% O2 and hyperbaric O2
Antidote used for digitalis toxicity
Digi-Bind (also need to stop digoxin, normalize K+, and lidocaine if pt. is arrhythmic)
Antidote used for beta agonist toxicity (eg. Metaproterenol)
Esmolol
Antidote for methotrexate toxicity
Leucovorin
Antidote for beta-blockers and hypoglycemia
Glucagon
Antidote useful for some drug induced Torsade de pointes
Magnesium sulfate
Antidote for hyperkalemia
sodium polystyrene sulfonate (Kayexalate)
Antidote for salicylate intoxication
Alkalinize urine, dialysis
Constant proportion of cell population killed rather than a constant number
Log-kill hypothesis
Treatment with cancer chemotherapy at high doses every 3-4 weeks, too toxic to be used continuously
Pulse therapy
Toxic effect of anticancer drug can be lessened by rescue agents
Rescue therapy
Drug used concurrently with toxic anticancer agents to reduce renal precipitation of urates
Allopurinol
Pyrimidine analog that causes "Thymine-less death" given with leucovorin rescue
5-flouracil (5-FU)
Drug used in cancer therapy causes Cushing-like symptoms
Prednisone
Side effect of Mitomycin
SEVERE myelosuppression
MOA of cisplatin
Alkylating agent
Common toxicities of cisplatin
Nephro and ototoxicity
Analog of hypoxanthine, needs HGPRTase for activation
6-mercaptopurine (6-MP)
Interaction with this drug requires dose reduction of 6-MP
Allopurinol
May protect against doxorubicin toxic by scavenging free radicals
Dexrazoxane
Blows DNA (breaks DNA strands), limiting SE is pulmonary fibrosis
Bleomycin
Bleomycin+vinblastine+etoposide+cisplatin produce almost a 100% response when all agents are used for this neoplasm
Testicular cancer
MOPP regimen used in Hodgkin's disease (HD)
Mechlorethamine+ oncovorin (vincristine)+ procarbazine, and prednisone
ABVD regimen used for HD, but appears less likely to cause sterility and secondary malignancies than MOPP
Adriamycin (doxorubicin) +bleomycin, vinblastine +dacarbazine
Regimen used for non-Hodgkin's lymphoma
COP (cyclophosphamide, oncovin(vincristine), and prednisone)
Regimen used for breast cancer
CMF (cyclophosphamide, methotrexate, and fluorouracil) and tamoxifen if ER+
Alkylating agent, vesicant that causes tissue damage with extravasation
Mechlorethamine
Anticancer drug also used in RA, produces acrolein in urine that leads to hemorrhagic cystitis
Cyclophosphamide
Prevention of cyclophosphamide induced hemorrhagic cystitis
Hydration and mercaptoethanesulfonate (MESNA)
Microtubule inhibitor that causes peripheral neuropathy, foot drop (eg. ataxia), and "pins and needles" sensation
Vincristine
Interact with microtubules (but unlike vinca which prevent disassembly of tubules), it stabilizes tubulin and cells remain frozen in metaphase
Paclitaxel (taxol)
Toxicities include nephrotoxicity and ototoxicity, leading to a severe interaction with aminoglycosides
Cisplatin
Agent similar to cisplatin, less nephrotoxic, but greater myelosuppression
Carboplatin
Converts asparagine to aspartate and ammonia, denies cancer cells of essential AA (asparagine)
L-asparaginase
Used for hairy cell leukemia; it stimulates NK cells
Interferon alpha
Anti-androgen used for prostate cancer
Flutamide (Eulexin)
Anti-estrogen used for estrogen receptor + breast cancer
Tamoxifen
Aromatase inhibitor used in breast cancer
Letrozole, anastrozole
Newer estrogen receptor antagonist used in advanced breast cancer
Toremifene (Fareston)
Some cell cycle specific anti-cancer drugs
Bleomycin, vinca alkaloids, antimetabolites (eg., 5-FU, 6-MP, methotrexate, etoposide)
Some cell cycle non-specific drugs
Alkylating agents (eg., mechlorethamine, cyclophosphamide), antibiotics (doxorubicin, daunorubicin), cisplatin, nitrosourea
Anti-emetics used in association with anti-cancer drugs that are 5-HT3 (serotonin receptor subtype ) antagonist
Odansetron, granisetron
Nitrosoureas with high lipophilicity, used for brain tumors
Carmustine (BCNU) and lomustine (CCNU)
Produces disulfiram-like reaction with ethanol
Procarbazine
Somatostatin (SRIF) analog used for acromegaly, carcinoid, glucagonoma and other GH producing pituitary tumors
Octreotide
Somatotropin (GH) analog used in GH deficiency (dwarfism)
Somatrem
GHRH analog used as diagnostic agent
Sermorelin
GnRH agonist used for infertility or different types of CA depending on pulsatile or steady usage respectively
Leuprolide
GnRH antagonist with more immediate effects, used for infertility
Ganirelix
Dopamine (DA) agonist (for Parkinson's disease), used also for hyperprolactinemia
Bromocriptine
Hormone inhibiting prolactin release
Dopamine
ACTH analog used for diagnosis of patients with corticosteroid abnormality
Cosyntropin
Synthetic analog of ADH hormone used for diabetes insipidus and nocturnal enuresis
Desmopressin (DDAVP)
SE of OCs
Increased thromboembolic events
Most widely used thyroid drugs such as Synthroid and Levoxyl contain
L-thyroxine (T4)
T3 compound less widely used
Cytomel
Anti-thyroid drugs
Thioamides, iodides, radioactive iodine, and ipodate
Thioamide agents used in hyperthyroidism
Methimazole and propylthiouracil (PTU)
Thioamide less likely to cross placenta, inhibits peripheral conversion of T4 to T3 in high doses, and should be used with extreme caution in pregnancy
PTU
PTU (propylthiouracil) MOA
Inhibits thyroid hormone synthesis by blocking iodination of the tyrosine residues of thyroglobulin
Can be effective for short term therapy of thyroid storm, but after several weeks of therapy causes an exacerbation of hyperthyroidism
Iodide salts
Dose may need to be increased during pregnancy or with Ocs due to increased TBG in plasma
Thyroxine
Permanently cures thyrotoxicosis, patients will need thyroid replacement therapy thereafter. Contraindicated in pregnancy
Radioactive iodine
Radio contrast media that inhibits the conversion of T4 to T3
Ipodate
Block cardiac adverse effects of thyrotoxicosis such as tachycardia, inhibits the conversion of T4 to T3
Beta-blockers such as propranolol
Vitamins containing iron should NOT be taken simultaneously with levothyroxine because
Iron deiodinates thyroxine
Thyroxine dose may need to be increased in hypothyroid patient during pregnancy because
Estogens increase maternal TBG
3 zones of adrenal cortex and their products
Glomerulosa (mineralocorticoids), fasciculata (glucocorticoid=GC), and reticularis (adrenal androgens)
Pneumonic for 3 zones of adrenal cortex
GFR
Used for Addison's disease, Congenital Adrenal Hyperplasia (CAH), inflammation, allergies, and asthma (as a local inhalation)
Glucocorticoids
Short acting GC's
Cortisone and hydrocortisone (equivalent to cortisol)
Intermediate acting GC's
Prednisone, methylprednisolone, prednisolone, and triamcinolone
Long acting GC's
Betamethasone, dexamethasone, and paramethasone
Mineralocorticoids
Fludrocortisone and deoxycorticosterone
Some side effects of corticosteroids
Osteopenia, impaired wound healing, inc. risk of infection, inc. appetite, HTN, edema, PUD, euphoria, psychosis, stria, thinning of skin
Period of time of therapy after which GC therapy will need to be tapered
5-7 days
Used for Cushing's syndrome (increased corticosteroid) and sometimes for adrenal function test
Metyrapone
Inhibits conversion of cholesterol to pregnenolone therefore inhibiting corticosteroid synthesis
Aminoglutethimide
Antifungal agent used for inhibition of all gonadal and adrenal steroids
Ketoconazole
Antiprogestin used as potent antagonist of GC receptor
Mifepristone
Diuretic used to antagonize aldosterone receptors
Spironolactone
Common SE of spironolactone
Gynecomastia and hyperkalemia
Slightly increased risk of breast cancer, endometrial cancer, heart disease (questionable), has beneficial effects on bone loss
Estrogen
Antiestrogen drugs used for fertility and breast cancer respectively
Clomiphene and tamoxifen
Common SE of tamoxifen and raloxifene
Hot flashes
Selective estrogen receptor modulator (SERM) used for prevention of osteoporosis and currently being tested for treatment of breast cancer (Stars study)
Raloxifene
Non-steroidal estrogen agonist causes clear cell adenocarcinoma of the vagina in daughters of women who used it during pregnancy
Diethylstilbestrol (DES)
Estrogen mostly used in oral contraceptives (OC)
Ethinyl estradiol and mestranol
Anti-progesterone used as abortifacient
Mifepristone (RU-486)
Constant low dose of estrogen and increasing dose of progestin for 21 days (last 5 days are sugar pills or iron prep)
Combination oral contraceptives (OC)
Oral contraceptive available in a transdermal patch
Ortho-Evra
Converted to more active form DHT by 5 alpha-reductase
Testosterone
5 alpha-reductase inhibitor used for benign prostatic hyperplasia (BPH) and male pattern baldness
Finasteride (Proscar and Propecia respectively)
Anabolic steroid that has potential for abuse
Nandrolone and stanozolol
Anti-androgen used for hirsutism in females
Cyproterone acetate
Drug is used with testosterone for male fertility
Leuprolide
Alpha cells in the pancreas
Produce glucagon
Beta cells in the pancreas
Produce insulin
Beta cells are found
Islets of Langerhans
Delta cells in the pancreas
Produce Somatostatin
Product of proinsulin cleavage used to assess insulin abuse
C-peptide
Exogenous insulin
Little C-peptide
Endogenous insulin
Normal C-peptide
Very rapid acting insulin, having fastest onset and shortest duration of action
Lispro (Humalog)
Rapid acting, crystalline zinc insulin used to reverse acute hyperglycemia
Regular (Humulin R)
Long acting insulin
Ultralente (humulin U)
Ultra long acting insulin, has over a day duration of action
Glargine (Lantus)
Major SE of insulin
Hypoglycemia
Important in synthesis of glucose to glycogen in the liver
GLUT 2
Important in muscle and adipose tissue for glucose transport across muscles and TG storage by lipoprotein lipase activation
GLUT 4
Examples of alpha-glucosidase inhibitors (AGI)
Acarbose, miglitol
MOA of AGI's
Act on intestine, delay absorption of glucose
SE of AGI's
Flatulence (do not use beano to tx), diarrhea, abdominal cramps
Alpha-glucosidase inhibitor associated with elevation of LFT's
Acarbose
Amino acid derivative
Nateglinide
MOA of nateglinide
Insulin secretagogue
Biguanide
Metformin
Drugs available in combination with metformin
Glyburide, glipizide, and rosiglitazone
MOA of metformin
Decreases hepatic glucose production and intestinal glucose absorption; increase insulin sensitivity
Most important potential SE of metformin
Lactic acidosis
Meglitinide
Repaglinide
MOA of repaglinide
Insulin release from pancreas; faster and shorter acting than sulfonylurea
First generation sulfonylurea
Chlorpropamide, tolbutamide, tolazamide, etc.
Second generation sulfonylurea
Glyburide, glipizide, glimepiride, etc.
MOA of both generations
Insulin release from pancreas by modifying K+ channels
Common SE of sulfonylureas, repaglinide, and nateglinide
Hypoglycemia
Sulfonylurea NOT recommended for elderly because of very long half life
Chlorpropamide
Thiazolidinediones
Pioglitazone, Rosiglitazone, Troglitazone (withdrawn/d from market)
Reason troglitazone was withdrawn from market
Hepatic toxicity
MOA of thiazolindinediones
Stimulate PPAR-gamma receptor to regulate CHO and lipid metabolism
SE of Thiazolindinediones
Edema, mild anemia; interaction with drugs that undergo CytP450 3A4 metabolism
Hyperglycemic agent that increases cAMP and results in glycogenolysis, gluconeogenesis, reverses hypoglycemia, also used to reverse severe beta-blocker overdose and smooth muscle relaxation
Glucagon
Available bisphosphonates
Alendronate, etidronate, risedronate, pamidronate, tiludronate, and zoledronic acid
MOA of Bisphosphonates
Inhibits osteoclast bone resorption
Only bisphosphonates available IV
Etidronate
Uses of bisphosphonates
Osteoporosis, Paget's disease, and osteolytic bone lesions, and hypercalcemia from malignancy
Major SE of bisphosphonates
Chemical esophagitis
Bisphosphonates that cannot be used on continuous basis because it caused osteomalacia
Etidronate
Used for prevention of postmenopausal osteoporosis in women
Estrogen (HRT-Hormone replacement therapy)
Increase bone density, also being tested for breast CA tx.
Raloxifene (SERM-selective estrogen receptor modulator)
Used intranasally and decreases bone resorption
Calcitonin (salmon prep)
Used especially in postmenopausal women, dosage should be 1500 mg
Calcium
Vitamin given with calcium to ensure proper absorption
Vitamin D
Disease caused by excess ergot alkaloids
St. Anthony's Fire
Endogenous substances commonly interpreted as histamine, serotonin, prostaglandins, and vasoactive peptides
Autocoids
Syndrome of hypersecretion of gastric acid and pepsin usually caused by gastrinoma; it is associated with severe peptic ulceration and diarrhea
Zollinger-Ellison Syndrome
Drug that causes contraction of the uterus
Oxytocin
Distribution of histamine receptors H1, H2, and H3
Smooth muscle; stomach, heart, and mast cells; nerve endings, CNS respectively
Prototype antagonist of H1 and H2 receptors
Diphenhydramine and cimetridine, respectively
1st generation antihistamine that is highly sedating
Diphendydramine
1st generation antihistamine that is least sedating
Chlorpheniramine or cyclizine
2nd generation antihistamines
Fexofenadine, loratadine, and cetirizine
Generation of antihistamine that has the most CNS effects
First generation due to being more lipid-soluble
Major indication for H1 receptor antagonist
Use in IgE mediated allergic reaction
Antihistamine that can be used for anxiety and insomnia and is not addictive
hydroxyzine (Atarax)
H1 antagonist used in motion sickness
Dimenhydrinate, meclizine, and other 1st generation
Most common side effect of 1st generation antihistamines
Sedation
Lethal arrhythmias resulting from concurrent therapy with azole fungals (metabolized by CYP 3A4) and these antihistamines which inhibit the 3A4 iso-enzyme.
Terfenadine and astemizole (have been removed from the market)
H2 blocker that causes the most interactions with other drugs
Cimetidine
Clinical use for H2 blockers
Acid reflux disease, duodenal ulcer and peptic ulcer disease
Receptors for serotonin (5HT-1) are located
Mostly in the brain, and they mediate synaptic inhibition via increased K+ conductance
5HT-1d agonist used for migraine headaches "
Sumatriptan, naratriptan, and rizatriptan
Triptan available in parenteral and nasal formulation
Sumatriptan
H1 blocker that is also a serotonin antagonist
Cyproheptadine
Agents for reduction of postpartum bleeding
Oxytocin, ergonovine and ergotamine
Agents used in treatment of carcinoid tumor
Ketanserin cyproheptadine, and phenoxybenzamine
5HT-3 antagonist used in chemotherapeutic induced emesis
Ondansetron, granisetron, dolasetron and alosetron
5ht-3 antagonist that has been associated with QRS and QTc prolongation and should not be used in patients with heart disease
Dolasetron
DOC of chemo induced nausea and vomiting
Odansetron
Drug used in ergot alkaloids overdose, ischemia and gangrene
Nitroprusside
Reason ergot alkaloids are contraindicated in pregnancy
Uterine contractions
SE of ergot alkaloids
Hallucinations resembling psychosis
Ergot alkaloid used as an illicit drug
LSD
Dopamine agonist used in hyperprolactinemia
Bromocriptine
Peptide causing increased capillary permeability and edema
Bradykinin and histamine
Mediator of tissue pain, edema, inactivated by ACE, and may be a contributing factor to the development of angioedema
Bradykinin
Drug causing depletion of substance P (vasodilator)
Capsaicin
Prostaglandins that cause abortions
Prostaglandin E1 (misoprostol) PGE2, and PGF2alpha
Difference between COX 1 and COX 2
COX 1 is found throughout the body and COX 2 is only in inflammatory tissue
Drug that selectively inhibits COX 2
Celecoxib and rofecoxib
Inhibitor of lipoxygenase
Zileuton
Major SE of zileuton
Liver toxicity
Inhibitor of leukotrienes (LTD4) receptors and used in asthma
Zafirlukast and montelukast
Used in pediatrics to maintain patency of ductus arteriosis
PGE1
Approved for use in severe pulmonary HTN
PGI2 (epoprostenol)
Prostaglandin used in the treatment impotence
Alprostadil
Irreversible, nonselective COX inhibitor
Aspirin
Class of drugs that reversibly inhibit COX
NSAIDS
Primary endogenous substrate for Nitric Oxidase Synthase
Arginine
MOA and effect of nitric oxide
Stimulates cGMP which leads to vascular smooth muscle relaxation
Long acting beta 2 agonist used in asthma
Salmeterol
Muscarinic antagonist used in asthma
Ipratropium
MOA action of cromolyn
Mast cell stabilizer
Methylxanthine derivative used as a remedy for intermittent claudication
Pentoxifylline
MOA of corticosteroids
inhibit phospholipase A2
SE of long term (>5 days) corticosteroid therapy and remedy
Adrenal suppression and weaning slowly, respectively
MOA of quinolones
Inhibit DNA gyrase
MOA of penicillin
Block cell wall synthesis by inhibiting peptidoglycan cross-linkage
Drug used for MRSA
Vancomycin
Vancomycin MOA
Blocks peptidoglycan synthesis
Type of resistance found with vancomycin
Point mutation
Meningitis prophylaxis in exposed patients
Rifampin
Technique used to diagnose perianal itching, and the drug used to treat it
Scotch tape technique and Mebendazole
Two toxicities of aminoglycosides
nephro and ototoxicity
DOC for Legionnaires' disease
Erythromycin
MOA of sulfonamides
Inhibit dihydropteroate synthase
Penicillins active against penicillinase secreting bacteria
Methicillin, nafcillin, and dicloxacillin
Cheap wide spectrum antibiotic DOC of otitis media
Amoxicillin
Class of antibiotics that have 10% cross sensitivity with penicillins
Cephalosporins
PCN active against pseudomonas
Carbenicillin, piperacillin and ticarcillin
Antibiotic causing red-man syndrome, and prevention
Vancomycin, infusion at a slow rate, and anti-histamines
Drug causes teeth discoloration
Tetracycline
MOA of tetracycline
Decreases protein synthesis by inhibiting 30S ribosome
Drug that causes gray baby syndrome and aplastic anemia
Chloramphenicol
Drug notorious for causing pseudomembranous colitis
Clindamycin
DOC for tx of pseudomembranous colitis
Metronidazole
Treatment of resistant pseudomembranous colitis
ORAL vancomycin
Anemia caused by trimethoprim
Megaloblastic anemia
Reason fluoroquinolones are contraindicated in children and pregnancy
Cartilage damage
DOC for giardia, bacterial vaginosis, pseudomembranous colitis, and trichomonas
Metronidazole
Treatment for TB patients (think RIPE)
Rifampin, Isoniazid, Pyrazinamide, and Ethambutol
Metronidazole SE if given with alcohol
Disulfiram-like reaction
Common side effect of Rifampin
Red urine discoloration
MOA of nystatin
Bind ergosterol in fungal cell membrane
Neurotoxicity with isoniazid (INH) prevented by
Administration of Vit. B6 (pyridoxine)
Toxicity of amphotericin
Nephrotoxicity
SE seen only in men with administration of ketoconazole
Gynecomastia
Topical DOC in impetigo
Topical mupirocin (Bactroban)
DOC for influenza A
Amantadine
DOC for RSV
Ribavirin
DOC for CMV retinitis
Ganciclovir
SE for ganciclovir
Neutro, leuko and thrombocytopenia
Anti-viral agents associated with Stephen Johnson syndrome
Nevirapine, amprenavir
HIV antiviral class known to have severe drug interactions by causing inhibition of metabolism
Protease inhibitors
Antivirals that are teratogens
Delavirdine, efavirenz, and ribavirin
Antivirals associated with neutropenia
Ganciclovir, zidovudine, saquinavir, and interferon
HIV med used to reduce transmission during birth
AZT (zidovudine)
Drug used for African sleeping sickness
Suramin
Drug used in Chagas disease
Nifurtimox
Cephalosporins able to cross the BBB
Cefuroxime (2nd generation) and Ceftazidime
Cephalosporins that do NOT cross BBB
Cefixime (3rd gen)
Drug used for N. gonorrhea in females
Ceftriaxone
Cephalosporin causes kernicterus in neonates
Ceftriaxone or cefuroxime
SE of INH
Peripheral neuritis and hepatitis
Aminoglycoside that is least ototoxic
Streptomycin
Drug used in exoerythrocytic cycle of malaria
Primaquine
Oral antibiotic of choice for moderate inflammatory acne
Minocycline
Drug of choice for leprosy
Dapsone
DOC for herpes and its MOA
Acyclovir; incorporated into viral DNA and chain termination
Anti-microbials that cause hemolysis in G6PD-deficient patients
Sulfonamides
MOA of erythromycin
Inhibition of protein synthesis at the 50s subunit of ribosome
Anti-biotic frequently used for chronic UTI prophylaxis
sulfamethoxazole/ trimethoprim
Lactam that can be used in PCN allergic patients
Aztreonam
SE of imipenem
Seizures
Anti-viral with a dose limiting toxicity of pancreatitis
Didanosine
Common side effect of hypnotic agents
Sedation
Occurs when sedative hypnotics are used chronically or at high doses
Tolerance
The most common type of drug interaction of sedative hypnotics with other depressant medications
Additive CNS depression
Benzodiazepines used to promote sleep
Temazpam, trizolam, flurazepam
Benzodiazepine used for anxiety
Alprazolam
Non-benzodiazepine used as an anxiolytic
Buspirone
Non-benzodiazepine used for sleep
Zolpidem
Major effect of benzodiazepines on sleep at high doses
REM is decreased
Neurologic SE of benzodiazepines
Anterograde amnesia
Reason benzos are used cautiously in pregnancy
Ability to cross the placenta
Main route of metabolism for benzodiazepines
Hepatic
Benzodiazepine that undergo extrahepatic conjugation (which are useful in older or hepatically impaired)
Lorazepam, oxazepam, and temazepam
MOA for benzodiazepines
increase the FREQUENCY of GABA-mediated chloride ion channel opening
Antidote to benzodiazepine overdose (antagonist that reverses the CNS effects)
Flumazenil
Benzodiazepine with useful relaxant effects in skeletal muscle spasticity of central origin
Diazepam
Benzodiazepine that has efficacy against absence seizures and in anxiety states, such as agoraphobia
Clonazepam
Benzodiazepines that are the most effective in the treatment of panic disorder
Alprazolam and Clonazepam
Benzodiazepine that is used for anesthesia
Midazolam
DOC for status epilepticus
Diazepam
Longer acting benzodiazepines used in the management of withdrawal states of alcohol and other drugs
Chlordiazepoxide and Diazepam
Agents having active metabolites, long half lives, and a high incidence of adverse effects
Diazepam, Flurazepam, chlordiazepoxide, and clorazepate
Barbiturates may precipitate this hematologic condition
Acute intermittent porphyria
Barbiturates decrease the effectiveness of many other drugs via this pharmacokinetics property
Liver enzyme INDUCTION
Barbiturates MOA
Increase the DURATION of GABA-mediated chloride ion channels
Barbiturate used for the induction of anesthesia
Thiopental
Site of action for zaleplon and zolpidem
Benzodiazepine receptor BZ1 (although are not considered benzodiazepines)
Good hypnotic activity with less CNS SE than most benzodiazepines
Zolpidem, zaleplon
Agent that is a partial agonist for the 5-HT1A receptor
Buspirone
Drug of choice for generalized anxiety disorder, NOT effective in acute anxiety
Buspirone
Agent that is metabolized to acetaldehyde by alcohol dehydrogenase and microsomal ethanol-oxidizing system (MEOS)
Ethanol
Agent with zero-order kinetics
Ethanol
Rate limiting step of alcohol metabolism
Aldehyde dehydrogenase
System that increases in activity with chronic exposure and may contribute to tolerance
MEOS
Agent that metabolize acetaldehyde to acetate
Aldehyde dehydrogenase
Agents that inhibit alcohol dehydrogenase
Disulfiram, metronidazole, certain sulfonylureas and cephalosporins
Agent used in the treatment of alcoholism, if alcohol is consumed concurrently, acetaldehyde builds up and results in nausea, headache, flushing, and hypotension
Disulfiram
The most common neurologic abnormality in chronic alcoholics
Peripheral neuropathy (also excessive alcohol use is associated with HTN, anemia, and MI)
Agent that is teratogen and causes a fetal syndrome
Ethanol
Agent that is the antidote for methanol overdose
Ethanol
Drug that inhibits alcohol dehydrogenase and is used in ethylene glycol exposure
Fomepizole
Most frequent route of metabolism
Hepatic enzymes
Mechanisms of action for Phenytoin, Carbamazepine, Lamotrigine
Sodium blockade
MOA for benzodiazepines and barbiturates
GABA-related targets
MOA for Ethosuximide
Calcium channels
MOA for Valproic acid at high doses
Affect calcium, potassium, and sodium channels
Drugs of choice for generalized tonic-clonic and partial seizures
Valproic acid and Phenytoin
DOC for febrile seizures
Phenobarbital
Drugs of choice for absence seizures
Ethosuximide and valproic acid
Drug of choice for myoclonic seizures
Valproic acid
Drugs of choice for status epilepticus
IV diazepam for short term (acute) treatment; phenytoin for prolonged therapy
Drugs that can be used for infantile spasms
Corticosteroids
Anti-seizure drugs used also for bipolar affective disorder (BAD)
Valproic acid, carbamazepine, phenytoin and gabapentin
Anti-seizure drugs used also for Trigeminal neuralgia
Carbamazepine
Anti-seizure drugs used also for pain of neuropathic orgin
Gabapentin
Anti-seizure agent that exhibits non-linear metabolism, highly protein bound, causes fetal hydantoin syndrome, and stimulates hepatic metabolism
Phenytoin
SE of phenytoin
Gingival hyperplasia, nystagmus, diplopia and ataxia
Anti-seizure agent that induces formation of liver drug-metabolism enzymes, is teratogen and can cause craniofacial anomalies and spina bifida
Carbamazepine
Agent that inhibits hepatic metabolism, is hepatotoxic and teratogen that can cause neural tube defects and gastrointestinal distress
Valproic acid
Laboratory value required to be monitored for patients on valproic acid
Serum ammonia and LFT's
SE for Lamotrigine
Stevens-Johnson syndrome
SE for Felbamate
Aplastic anemia and acute hepatic failure
Anti-seizure medication also used in the prevention of migraines
Valproic acid
Carbamazepine may cause
Agranulocytosis
Anti-seizure drugs used as alternative drugs for mood stabilization
Carbamazepine, gabapentin, lamotrigine, and valproic acid
MOA of general anesthetics
Most are thought to act at GABA-A receptor - chloride channel
Inhaled anesthetic with a low blood/gas partition coefficient
Nitrous oxide
Inversely related to potency of anesthetics
Minimum alveolar anesthetic concentration (MAC)
Inhaled anesthetics metabolized by liver enzymes which has a major role in the toxicity of these agents
Halothane and methoxyflurane
Most inhaled anesthetics SE
Decrease arterial blood pressure
Inhaled anesthetics are myocardial depressants
Enflurane and halothane
Inhaled anesthetic causes peripheral vasodilation
Isoflurane
Inhaled anesthetic that may sensitize the myocardium to arrhythmogenic effects of catecholamines and has produced hepatitis
Halothane
Inhaled anesthetic, less likely to lower blood pressure than other agents, and has the smallest effect on respiration
Nitrous oxide
Fluoride released by metabolism of this inhaled anesthetic may cause renal insufficiency
Methoxyflurane
Prolonged exposure to this inhaled anesthetic may lead to megaloblastic anemia
Nitrous oxide
Pungent inhaled anesthetic which leads to high incidence of coughing and vasospasm
Desflurane
DOC for malignant hyperthermia that may be caused by use of halogenated anesthetics
Dantrolene
IV barbiturate used as a pre-op anesthetic
Thiopental
Benzodiazepine used adjunctively in anesthesia
Midazolam
Benzodiazepine receptor antagonist, it accelerates recovery from benzodiazepine overdose
Flumazenil
This produces "dissociative anesthesia", is a cardiovascular stimulant which may increases intracranial pressure, and hallucinations occur during recovery
Ketamine
Opioid associated with respiratory depression, but is used in high risk patients who may not survive full general anesthetia
Fentanyl
State of analgesia and amnesia produced when fentanyl is used with droperidol and nitrous oxide
Neuroleptanesthesia
Produces both rapid anesthesia and recovery, has antiemetic activity and commonly used for outpatient surgery, may cause marked hypotension
Propofol