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238 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
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
Inducers of Cytochrome P450 (CYP450)
Barbiturates, phenytoin, carbamazepine, and rifampin
Inhibitors of CYP450
Cimetidine, ketoconazole, erythromycin, isoniazid and grapefruit
Products of Phase II conjugation
Glucuronate, acetic acid, and glutathione sulfate
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 times (volume of distribution divided by bioavailability)
Loading dose (Cp*(Vd/F))
Concentration in the plasma times (clearance divided by bioavailability)
Maintenance dose (Cp*(CL/F))
Strength of interaction between drug and its receptor
Selectivity of a drug for its receptor
Amount of drug necessary to elicit a biologic effect
Ability of drug to produce a biologic effect
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
MOA utilizes ligand gated ion channels
Benzodiazepines and calcium channel blockers
Median effective dose required for an effect in 50% of the population
Median toxic dose required for a toxic effect in 50% of the population
Dose which is lethal to 50% of the population
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
Antidote used for anticholinergic poisoning
Antidote used for organophosphate/anticholinesterase poisoning
Atropine, pralidoxime (2-PAM)
Antidote used for iron salt toxicity
Antidote used for acetaminophen (APAP) toxicity
N-acetylcysteine (Mucomyst)
Antidote for arsenic, mercury, lead, and gold poisoning
Antidote used in poisonings: copper (Wilson's disease), lead, mercury, and arsenic
Antidote used for heparin toxicity
Antidote used for warfarin toxicity
Vitamin and Fresh frozen plasma (FFP)
Antidote for tissue plasminogen activator (t-PA), streptokinase
Aminocaproic acid
Antidote used for methanol and ethylene glycol
Antidote used for opioid toxicity
Naloxone (IV), naltrexone (PO)
Antidote used for benzodiazepine toxicity
Antidote used for tricyclic antidepressants (TCA)
Sodium bicarbonate
Antidote used for carbon monoxide poisoning
100% O2 and hyperbaric O2
Antidote used for digitalis toxicity
Digibind (also need to d/c digoxin, normalize K+, and lidocaine if pt. Is arrhythmic)
Antidote used for beta agonist toxicity (eg. Metaproterenol)
Antidote for methotrexate toxicity
Antidote for beta-blockers and hypoglycemia
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
Pyrimidine analog that causes "Thiamine-less death" given with leucovorin rescue
5-flouracil (5-FU)
Drug used in cancer therapy causes Cushing-like symptoms
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
May protect against doxorubicin toxic by scavenging free radicals
Blows DNA (breaks DNA strands), limiting SE is pulmonary fibrosis
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
Anticancer drug also used in RA, produces acrolein in urine that leads to hemorrhagic cystitis
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
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
Agent similar to cisplatin, less nephrotoxic, but greater myelosuppression
Converts asparagine to aspartate and ammonia, denies cancer cells of essential AA (asparagine)
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
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
Somatostatin (SRIF) analog used for acromegaly, carcinoid, glucagonoma and other GH producing pituitary tumors
Somatotropin (GH) analog used in GH deficiency (dwarfism)
GHRH analog used as diagnostic agent
GnRH agonist used for infertility or different types of CA depending on pulsatile or steady usage respectively
GnRH antagonist with more immediate effects, used for infertility
Dopamine (DA) agonist (for Parkinson's disease), used also for hyperprolactinemia
Hormone inhibiting prolactin release
ACTH analog used for diagnosis of patients with corticosteroid abnormality
Synthetic analog of ADH hormone used for diabetes insipidus and nocturnal enuresis
Desmopressin (DDAVP)
Most widely used thyroid drugs such as Synthroid and Levoxyl contain
L-thyroxine (T4)
T3 compound less widely used
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 (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
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
Block cardiac adverse effects of thyrotoxicosis such as tachycardia, inhibits the conversion of T4 to T3
Beta-blockers such as propranolol
3 zones of adrenal cortex and their products
Glomerulosa (mineralocorticoids), fasciculata (glucocorticoid=GC), and reticularis (adrenal androgens)
Pneumonic for 3 zones of adrenal cortex
Used for Addison's disease, Congenital Adrenal Hyperplasia (CAH), inflammation, allergies, and asthma (as a local inhalation)
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
Fludrocortisone and deoxycorticosterone
Some side effects of corticosteroids
Osteopenia, impaired wound healing, inc. risk of infection, inc. appetite, HTN, edema, PUD, euphoria, psychosis
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
Inhibits conversion of cholesterol to pregnenolone therefore inhibiting corticosteroid synthesis
Antifungal agent used for inhibition of all gonadal and adrenal steroids
Antiprogestin used as potent antagonist of GC receptor
Diuretic used to antagonize aldosterone receptors
Common SE of spironolactone
Gynecomastia and hyperkalemia
******Slightly increased risk of breast cancer, endometrial cancer, heart disease (questionable), has beneficial effects on bone loss
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)
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
Converted to more active form DHT by 5 alpha-reductase
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
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
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
Important in synthesis of glucose to glycogen in the liver
Important in muscle and adipose tissue for glucose transport across muscles and TG storage by lipoprotein lipase activation
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
Amino acid derivative
MOA of nateglinide
Insulin secretagogue
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
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
Sulfonylurea NOT recommended for elderly because of very long half life
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
Available bisphosphonates
Alendronate, etidronate, risedronate, pamidronate, tiludronate, and zoledronic acid
MOA of Bisphosphonates
Inhibits osteoclast bone resorption
Only bisphosphonates available IV
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
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
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
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
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 impromidine respectively
1st generation antihistamine that is highly sedating
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
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
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
H1 blocker that is also a serotonin antagonist
5HT2 antagonist mediate synaptic excitation in the CNS and smooth muscle contraction
Ketanserin, cyproheptadine, and ergot alkaloids (partial agonist of alpha and serotonin receptors)
Agents for reduction of postpartum bleeding
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
DOC of chemo induced nausea and vomiting
Drug used in ergot alkaloids overdose, ischemia and gangrene
Reason ergot alkaloids are contraindicated in pregnancy
Uterine contractions
SE of ergot alkaloids
Hallucinations resembling psychosis
Ergot alkaloid used as an illicit drug
Dopamine agonist used in hyperprolactinemia
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
Drug causing depletion of substance P (vasodilator)
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, valdecoxib, and rofecoxib
Inhibitor of lipoxygenase
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
Approved for use in severe pulmonary HTN
PGI2 (epoprostenol)
Prostaglandin used in the treatment impotence
Irreversible, nonselective COX inhibitor
Class of drugs that reversibly inhibit COX
Primary endogenous substrate for Nitric Oxidase Synthase
MOA and effect of nitric oxide
Stimulates cGMP which leads to vascular smooth muscle relaxation
Long acting beta 2 agonist used in asthma
Muscarinic antagonist used in asthma
MOA action of cromolyn
Mast cell stabilizer
Enzyme which theophylline inhibits