Pharmacology One-Liners 2 Flashcards
First-line drugs for acute gout
Indomethacin, naproxen
NSAID avoided in gout because low doses increase uric acid levels
Aspirin
Mechanism of action of colchicine
Inhibits microtubules assembly, decreases leukocyte migration, and phagocytosis
Side effects of colchicine
Diarhhea, liver toxicity, myelosuppression
Agents that inhibit xanthine oxidases and used to treat chronic gout
Allopurinol, febuxostat
Recombinant uricase that enhances uric acid metabolism and indicated for gout refractory to conventional therapy
Pegloticase
DMARDs are slow-acting drugs for this indication
Rheumatic diseases
1st line for rheumatic arthritis for most patients
Low-dose methotrexate
Dose-limiting toxicity of methotrexate
Myelosuppression
A mixture of two agents with one agent active for rheumatic disease and the other for inflammatory bowel disease
Sulfasalzine
Agent used to treat chronic gout by increasing uric acid excretion through inhibition of URAT1 anion transporter
Probenecid
Alternative to methotrexate as 1st line for rheumatoid arthritis through inhibition of dihydroorotate dehydrogenase, which leads to decreased pyrimidine synthesis
Leflunomide
Side effect of penicillamine
Hypersensitivity (rash), nephrotoxicity, myopathy, myelosuppression
Anti-malarial drug used in rheumatoid arthritis
Hydroxychloroquine
Side effect of hydroxychloroquine
Retinopathy
Two drugs that bind and prevent action of tumor necrosis factor alpha (TNF-alpha)
Infliximab and etanercept
Neuromuscular blocking drugs
Structurally related to acetylcholine, used to produce muscle paralysis in order to facilitate surgery or artificial ventilation. Full doses lead to respiratory paralysis and require ventilation
Class of agents that block acetylcholine receptors at motor endplates and its effects can be reversed by cholinesterase inhibitors
Nondepolarizing blockers
Tubocurarine
Non-depolarizing neuromuscular blocker with long duration of action and is most likely to cause histamine release
Two non-depolarizing blockers that undergo Hofmann elimination, which is useful for patients with renal and hepatic deficiency
Atracurium, cisatracurium
Pancuronium
Non-depolarizing neuromuscular blocker with long duration of action that can block muscarinic receptor in the heart
These drugs strongly potentiate and prolong effect of neuromuscular blockers
Inhalation anesthetics (isoflurane), antibiotics (aminoglycosides, tetracyclines)
Succinylcholine
Depolarizing blocker that causes muscle relaxation and paralysis and can cause postoperative muscle pain
Two life-threatening side effects of succinylcholine
Hyperkalemia, malignant hyperthermia
Dantrolene
Drug for treating malignant hyperthermia associated with drug-drug interaction between halogenated anesthetics and depolarizing blocker
During Phase I depolarizing block this class of agents enhance muscle paralysis, but during Phase II block they may reverse muscle paralysis
Cholinesterase inhibitors
Neostigmine
Drug of choice for reversal of non-depolarizing neuromuscular blockade
Mechanism of action of cromolyn
Prevent mast cell degranulation (by blocking opening of Cl- channels)
Which enzyme does theophylline inhibit?
Phosphodiesterase
Somatropin
Growth hormone analog used in growth hormone deficiency
Octreotide
Somatostatin analog used for acromegaly, carcinoid, glucagonoma, and other growth hormone-producing pituitary tumors
Leuprolide
Gonadotropin-releasing hormone analog used for infertility (pulsatile administration) or suppression of gonadotropin production (continuous administration)
Ganirelix
Competitive antagonists at gonadotropin releasing hormone receptors used to prevent LH surger during controlled ovarian hyperstimulation
Bromocriptine
Ergot dopamine agonist used to suppress prolactin release
Cosyntropin
Synthetic human corticotropin used for diagnosis of adrenal insufficiency
Oxytocin
Agent used to stimulate uterine contraction and labor, milk letdowns, and control postpartum bleeding
Levothyroxine (T4)
Agent of choice for the treatment of hypothyroidism
Liothyronine (T3)
An isomer of T3 which may be used in myxedema coma
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 indicated for pregnant women in 1st trimester
Propylthiouracil (PTU)
Propylthiouracil mechanism of action
Inhibits thyroid peroxidase
Can be effective for short term therapy of thyroid storm, but after several weeks of therapy causes an exacerbation of hyperthyroidism
Iodide salts (potassium iodide)
Radioactive iodine
Permanently cures thyrotoxicosis, patients will need thyroid replacement therapy thereafter. Contraindicated in pregnancy
Used for symptomatic treatment of thyrotoxicosis by blocking cardiac adverse effects
Beta-blockers such as propranolol and esmolol
Glucocorticoids
Used for Addison’s disease, congenital adrenal hyperplasia inflammation, immune suppresion, and asthma
Two short-acting glucocorticoids
Hydrocortisone (cortisol), cortisone
Four intermediate-acting glucocorticoids
Prednisone, prednisolone, methylprednisolone, and triamcinolone
Two long-acting glucocorticoids
Betamethasone, dexamethasone
Two glucocorticoids with mineralocorticoid action
Fludrocortisone and deoxycorticosterone
Side effects of corticosteroids
Iatrogenic Cushing’s syndrome, hyperglycemia, impaired wound healing, osteoporosis, peptic ulcers, myopathy, adrenal suppression (>2 week treatment)
Aminoglutethimide
Inhibits conversion of cholesterol to pregnenolone therefore inhibiting corticosteroid synthesis
Ketoconazole
Antifungal agent used to inhibit adrenal and gonadal steroid synthesis
Metyrapone
Seelctive inhibitor of 11-hydroxylation and interferes with cortisol and corticosterone synthesis; used for adrenal function tests and is the only adrenal-inhibiting medication that can be administered to pregnant women with Cushing’s syndrome
Mifepristone (RU486)
Glucocorticoid receptor antagonist that is used as an abortifacient due to its strong antiprogestin activity
Three rapid-acting insulin used for postprandial glycemia
Aspart, lispro, glulisine
Short-acting insulin used intravenously for ketoacidosis
Regular insulin
Intermediate-acting insulin with variable pharmacokinetics; use is mostly replaced by long-acting insulin
Neutral protamine Hagedorn (NPH) insulin
Two long-acting insulin preparations that provide basal glycemia control
Glargine, detemir
Major side-effect of insulin
Hypoglycemia
Tolbutamide
First generation sulfonylurea that is safest for elderly diabetics due to its short half-life
Chlorpropamide
First generation sulfonylurea contraindicated in elderly diabetics because of very long half-life
Three second generation sulfonylureas
Glyburide, glipizide, glimepride
Mechanism of action of sulfonylureas
Close K+ channels, depolarize cell, open voltage-gated Ca2+ channels, release insulin
Common side effect of first-generation sulfonylureas
Disulfiram-like reactions with alcohol use
Common side effect of second-generation sulofnylureas
Hypoglycemia
Repaglinide
A meglitinide insulin secretagogue that has no sulfur in its structure and may be used in type 2 diabetics with sulfonylurea allergy
Nateglinide
A D-phenylalanine derivative insulin secretagogue that is useful for type 2 diabetics with very reduced renal function
Mechanism of action of repaglinide and nateglinide
Close K+ channels, depolarize cell, open voltage-gated Ca2+ channels, release insulin
First line drug used for treatment of Type 2 diabetes
Metformin
Mechanism of action of metformin
decreased gluconeogeesnis, increased peripheral glucose uptake; increase insulin sensitivity
Most serious side effect of metformin
Lactic acidosis
Two thiazolidinediones
Pioglitazone, rosiglitazone
Mechanism of action of thiazolidinediones
Activate PPAR-gamma, increased transcription of insulin-responsive genes, increased GLUT4 glucose transporter, increased insulin sensitivity
Side effect of thiazolidinediones
Weight gain, edema, heart failure, hepatotoxicity
Two alpha-glucosidase inhibitors
Acarbose, miglitol
Mechanism of action of alpha-glucosidase inhibitors
Act on intestine, delay digestion and absorption of glucose
Side effect of alpha-glucosidase inhibitors
Flatulence, diarrhea, abdominal cramps
Pramlintide
Amylin analog that delays gastric emptying and suppresses glucagon release
Two glucagon-like polypeptide-1 (GLP-1) analogs that increase insulin secretion and suppress postprandial glucagon release
Exenatide, liraglutide
Three dipeptidyl peptidase-4 (DPP-4) inhibitors that reduce breakdown of glucagon-like polypeptide-1, resulting in increased insulin secretion and suppress postprandial glucagon release
Sitagliptin, saxagliptin, linagliptin
Bisphosphonates
Alendronate and -dronates
Mechanism of action of bisphosphonates
Inhibits osteoclast activity and prevent bone resorption
Uses of bisphosphonates
Osteoporosis, Paget’s disease, hypercalcemia
Major side effects of bisphosphonates
Corrosive esophagitis, osteonecrosis of the jaw
Etidronate
First generation bisphosphonate when used long-term causes osteomalacia
May be used intranasally to decrease bone resorption
Calcitonin (salmon prep)
Vitamin given with calcium to ensure proper absorption
Vitamin D
Its use can increase risk of endometrial and breast cancer, cause postmenopausal uterine bleeding, but can stabilize bone mineral loss
Estrogen
Antiestrogen drug used for treatment of infertility in anovulatory women
Clomiphene
Tamoxifen
Selective estrogen receptor modulator most commonly used for treatment of breast cancer
Raloxifine
Selective estrogen receptor modulator used for prevention of osteoporosis and invasive breast cancer
Common side effect of tamoxifen and clomiphene
Hot flushes
Two estradiol derivatives with higher oral bioavailability and longer half-lives that are primarily used as oral contraceptives
Ethinyl estradiol and mestranol
Testosterone
Androgen receptor agonist used to treat hypogonadism and promote secondary sex characteristics
Finasteride
5 alpha-reductase inhibitor used for benign prostatic hyperplasia and male patter baldness
Danazol
Partial androgen agonist used for endometriosis and hereditary angioedema
Flutamide
Androgen receptor antagonist used to treat prostate cancer
Cyproterone
Androgen receptor antagonist used for hirsutism in females
Autacoids
A class of endogenous substances that include histamine, serotonin, prostaglandins, vasoactive peptides that work in autocrine or paracrine manner
Two peptides that increase capillary permeability and edema
Bradykinin and histamine
Distribution of H1 histamine receptors
Smooth muscle and mast cells
Distribution of H2 histamine receptors
Stomach, heart, and mast cells
Distribution of H3 histamine receptors
Nerve endings, CNS
Most common side effect of 1st generation antihistamines
Sedation, anticholinergic
Dephenhydramine
1st generation antihistamine that is highly sedating
Chlorpheniramine
1st generation antihistamine that is least sedating
Major indication for H1 antihistamines
IgE mediated allergic reaction (allergic rhinitis, urticaria)
Antihistamine that is indicated for allergies, motion sickness, and insomnia
Diphenhydramine
Antihistamine with motion sickness as the only indication
Dimenhydrinate
Three 2nd generation antihistamines
Fexofenadine, loratadine, and cetirizine
H2 antagonist that causes the most interactions with other drugs
Cimetidine
Indication for H2 antagonists
Acid reflux disease, duodenal ulcer and peptic ulcer disease
Location of serotonin type-1 (5HT-1) receptors
Mostly in the brain
Buspirone
5HT-1A receptor partial agonist indicated for generalized anxiety disorder; due to longer onset of action, is less effective for acute anxiety
5HT-1D/1B agonist used for migraine headaches
Sumatriptan and -triptans
Ergotaimne
Ergot alkaloid indicated for migraine headaches
Reason ergot alkaloids are contraindicated in pregnancy
Uterine contractions
Two side effects of ergot alkaloids
Prolonged vasospasm and hallucinations resembling psychosis
Two drugs that may be used off-label for ischemia and gangrene caused by ergot alkaloids overuse
Nitroprusside, nitroglycerin
Serotonin receptor responsible for serotonin syndrome
5HT2