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81 Cards in this Set
- Front
- Back
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Short acting insulins?
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insulin, lispro
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intermediate insulins?
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NPH
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long acting insulins?
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lente, ultralente
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MOA of insulin?
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liver (increased glucose stored as glycogen) Muscle (increased glycogen and protein synth, K uptake) Fat (aids TG storage)
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Uses of insulin other than DM1?
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life threatening hyperkalemia and stress induced hyperglycemia
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Insulin toxicity?
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hypoglycemi, hypersensitivity rxn (very rare)
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Name the first generation sulfonylureas.
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tolbutamide, chlorpropamide
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name the second generation sulfonylureas.
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glyburide, glimeperide, glipizide
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MOA of sulfonylureas.
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close K channel in beta cell membrane so cell depolarizes…triggers insulin release via increased Ca influx
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Are sulfonylureas good for DM1, DM2 or both?
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DM2. (useless in DM1 b/c needs some islet fxn)
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First generation sulfonylureas toxicities?
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disulfiram-like effects
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Second generation sulfonylurea toxicity?
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hypoglycemia
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What class of drugs is metformin?
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biguanide
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Probable MOA of metformin?
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decreased GNG, increased glycolysis, decreased serum glucose
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Metformin for DM1, DM2 or both?
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both
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Metformin toxicity?
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lactic acidosis (contraindicated in renal insufficiency, CHF, elderly)
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MOA of glitazones?
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increased target cell response to insulin
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Glitazones, DM1, DM2 or both?
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DM2
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Glitazone toxicities/
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weight gain, CHF (fluid retention), (troglitazone is hepatotoxic)
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name two alpha glucosidase inhibitors.
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acarbose, miglitol
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alpha glucosidase inhibitor MOA?
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inhibit intestinal brush border alpha glucosidases (delayed sugar hydrolysis and glucose absorption lead to decreased postpradial hyperglycemia)
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alpha glucosidase inhibitor toxicity?
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flatulence
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Orlistat MOA?
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alters fat metabolism by inhibiting pancreatic lipases
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Indications for orlistat?
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long term obesity management
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Orlistat toxicities?
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steatorrhea, GI discomfort, reduced absorption of fat soluble vitamins, HA
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Sibutramine MOA?
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sympathomimetic SNRI
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Indication for sibutramine?
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short-term and long term obesity management
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Sibutramine toxicity?
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HTN, tachycardia
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Propylthiouracil, methimazole MOA?
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inhibit organification and coupling of thyroid hormone synthesis. Propylthiouracil also decreases peripheral conversion of T4 to T3
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Indications for propylthiouracil or methimazole?
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hyperthyroidism
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Toxicities of propylthiouracil and methimazole?
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skin rash, agranulocytosis (rare), aplastic anemia
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Indication for somatostatin?
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GH deficiency, turner's syndrome
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Indication for octreotide?
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acromegaly, carcinoid, gastrinoma, glucagonoma
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Indication for oxytocin?
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stimulates labor, uterine contractions, milk let-down; controls uterine hemorrhage
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Indication for desmopressin?
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Central (not nephrogenic) DI
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Uses of levothyroxine, triiodothyroxine?
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hypothyroidism, myxedema
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Levothyroxine, triiodothyroxine toxicity?
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tachycardia, heat intolerance, tremors
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What kind of drug is triamcinolone?
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glucocorticoid
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MOA of glucocorticoids?
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decreased production of leukotrienes/prostaglandins by inhibiting PLA2 and COX-2 expression
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Uses of glucocorticoids?
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addison's, inflammation, immune suppression, asthma
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Glucocorticoid toxicity?
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iatrogenic cushings (buff hump, moon facies, truncal obesity, muscle wasting, thin skin, easy bruisability, osteoporosis, adrenocortical atrophy, peptic ulcers)
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Aminoglutethimide
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-general steroidogenesis antagonist
block steroidogenesis by inhibiting P450scc -also inhibits other enzymes -used to reduce gonadal hormones in breast cancer patients -used to reduce adrenal cortical hormones in adrenal carcinoma -not complete inhibition, therefore cortisone added to block elevations in ACTH |
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Mitotane
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-general adrenocorticoid antagonist
o,p’-DDD (isomer of DDT) -selective toxicity for adrenal cortex -sometimes used as anti-tumor agent for adrenal carcinoma -MOA not understood; causes mitochondrial degenerate -need life-long GC and mineralocorticoid after mitotane use -high incidence of adverse effects -40% - CNS depression; 15% skin rashes; 80% GI disturbances |
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Metyrapone
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-a cortisol synthesis antagonist
-inhibits 11beta-hydroxylase (P450-11beta), so blocks cortisol synthesis -administered orally -used for diagnosis of HPA axis function -has been used for Cushing’s syndrome -dizziness and GI disturbance are acute adverse effect -elevated mineralocorticoids and androgens with chronic use |
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Ketoconazole: another steroidogenesis antagonist
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-another steroidogenesis antagonist
-antifungal agent that inhibits glucocorticoid synthesis at higher doses -blocks P450scc and most other biosynthetic enzymes -used in Cushing’s syndrome |
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Trilostane
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-steroid hormone antagonist
reversible inhibitor of 3-HSD -blocks cortisol and aldosterone synthesis -used when more definitive treatment cannot be used -used orally -not extensively use because response to drug disappointing |
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LEP
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early onset severe obesity; hyperphagia
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LEPR
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early onset obesity; moderate growth hormone impairment
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POMC
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early-onset obesity; ACTH deficiency
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PC-1
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extreme childhood obesity; ACTH/cortisol deficiency
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MC4R
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childhood onset obesity w/ hyperphagia; also hyperinsulinemia; 2% of obesity
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NTRK2
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severe hyperphagic obesity; LD & complex developmental abnormalities
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Phentermine
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NE mimetic
Short-term Satiety Stimulator |
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Diethylpropion
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NE mimetic
Short-term Satiety Stimulator |
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Sibutramine
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NE/5-HT reuptake inhibitor
Long-term Satiety stimulator |
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Orlistat (OTC)
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Lipase inhibitor
Malabsorption inhibitor |
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Levothyroxin (T4)
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Plasma 1/2 5-7 days
Long duration |
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Liothyronine (T3)
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Plasma 1/2 24 hours
Short duration |
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Liotrix (T4/T3; 4:1)
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Plasma 1/2 5-7 days
Long duration |
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Dessicated Thyroid
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Plasma 1/2 like T4 (5-7 days)
Long duration |
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Sibutramine (Meridia)
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approved for use for up to 2 year, DEA Schedule IV
appetite suppressant MOA - satiety enhancer via blockade of serotonin & NE reuptake in CNS |
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Sibutramine side effects
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CV-increased BP and HR
Contraindications: Severe renal impairment or severe hepatic dysfunction, uncontrolled or poorly controlled hypertension, patients with history of coronary artery disease, congestive heart failure, arrhythmias or stroke, or concomitant use of MAO inhibitor. |
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Subutramine interactions
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i. Selective serotonin reuptake inhibitors (SSRIs)
(e.g., Prozac®) Could have additive effects Serotonin syndrome(incoordination, myoclonus hyperreflexia, tremor, sweating, anxiety, agitation, hallucinations) ii. Monoamine oxidase inhibitors iii. Sympathomimetics iv. Cytochrome P450 3A4 inhibitors - (e.g. ketoconozole (antifungal) or erythromycin) |
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Sympathomimetics
-Prototype |
Phentermine
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Sympathomimetics
-Examples and MOA |
iv. Phentermine (Ionamin®) & Diethylpropion
b. MOA- affecting catecholamine release &/or mimicking catecholamines at peripheral & central sites. Effects both energy expenditure & feeding signals. For weight loss |
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Phentermine
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d. Approved for short-term use (up to 12 weeks)
e. Adverse effects - dry mouth, sleep interference, agitation, hypertension, tachycardia f. Contraindication: cardiac or vascular disease, hypertension, hyperthyroidism |
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Orlistat
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Pancreatic/gastric Lipase Inhibitor
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Orlistat MOA
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MOA: pancreatic & gastric lipases required for hydrolysis of triacylglycerols to free fatty acids & monoacylglycerols for absorption by intestines.
Orlistat potently inhibits both lipases (functionally irreversible), thus limiting hydrolysis & therefore absorption of dietary fats & causing their excretion. |
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Orlistat Pharmacokinetics:
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a. Not effective unless taken at the time of a meal
b. Not absorbed (<1%) by gut |
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Orlistat
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inhibits dietary fat absorption by 30%
decreases plasma lipids by 10% Improved glycemic control |
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Orlistat Adverse Effects
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a. Potential mal-absorption of hydrophobic vitamins (A, D, E and -carotene in particular) - (use multivitamin supplementation taken more than 2 hr before or after Orlistat use)
b. GI: rectal incontinence, oily stools (intensified with high fat meal), flatulence i. Majority of GI adverse effects diminish (i.e., transient ii. decreased with low fat diet (can act as an incentive to minimize fat in diet) |
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Orlistat Contraindications and interactions
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Contraindications: Not advised for pregnant or nursing women, children, adults > 65 yrs, people with gallbladder or chronic food-absorption problems.
Drug-drug interactions - Hydrophobic vitamins mal-absorption. No known effects on absorption of other drugs by gut. |
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Key Drugs/Drug List
-Appetite Suppressants -Nutrient Absorption Inhibitor |
Appetite suppressants:
Serotonin/Norepinephrine Reuptake Inhibitor: Sibutramine (Meridia) Sympathomimetics: Phentermine (Fastin®, Ionamin®) & Diethylpropion Nutrient Absorption Inhibitor: -Orlistat (Xenica; OTC version - Alli) |
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Propylthiouracil and Methimazole
-Actions |
inhibits thyroid peroxidase
-blocks organification of iodide -blocks coupling of iodotyrosines -does NOT affect iodide uptake or hormone release! -propylthiouracil inhibits peripheral conversion of T4 to T3 by iodothyronine 5’-deiodinase-1 |
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Propylthiouracil and Methimazole
-accumulates |
accumulates in thyroid for longer duration of action
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Propylthiouracil and Methimazole
-uses |
Hyperthyroidism
-Graves disease until remission -preparation for surgery or 131I- ablation Treatment of thyroid storm |
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Propylthiouracil and Methimazole
-toxicity |
Rash and fever
Agranulocytosis (0.3-0.6% incidence) |
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Thioamides
-site of inhibition |
Oxidation of iodide to molecular iodine
Coupling of iodotyrosine |
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propylthiouracil
-site of inhibition |
Deiodination of T4 to T3
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Iodide (high doses)
-site of inhibition |
T4/T3 release
Organification of iodine Coupling of iodotyrosine |
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glucocorticoids and
beta-blockers -site of inhibition |
Deiodination of T4 to T3
Symptomatic sites |
