Pharmacology One-Liners

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Basic Pharmacokinetics
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
Metabolism
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))
Pharmacodynamics
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
Antidotes and agents used in drug overdose
Antidote used for lead poisoning: Dimercaprol, EDTA
Antidote used for cyanide poisoning: Nitrites
Antidote used for anticholinergic poisoning: Physostigmine
Antidote used for organophosphate/anticholinesterase poisoning: Atropine, pralidoxime (2-PAM)
Antidote used for iron salt toxicity: Deferoxamine
Antidote used for acetaminophen (APAP) toxicity: N-acetylcysteine (Mucomyst)
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 toxicity: Protamine
Antidote used for warfarin toxicity: Vitamin K and Fresh frozen plasma (FFP)
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: Digibind (also need to d/c 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
Cancer Chemotherapy
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 "Thiamine-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
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
Endocrine drugs: hypothalamic and pituitary hormones
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)
Thyroid and anti-thyroid drugs
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
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
Adrenocorticosteroid and adrenocortical antagonists
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
Period of time of therapy after which GC therapy will need to be tapered: 5-7 days
Inhibitors of corticosteroids biosynthesis
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
Gonadal hormones and inhibitors
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
Pancreatic hormones, antidiabetics, and hyperglycemics
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
Drugs used in bone homeostasis
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
Drugs with important actions on smooth muscle
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 impromidine 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
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: 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, valdecoxib, 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

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