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Weight Loss Drugs
Pharmacology Module 4
86
Medical
Graduate
07/28/2009

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Cards

Term
4 Anticonvulsants that cause weight gain
Definition
Carbamazepine
Gabapentin,
Pregabalin,
Valproic acid,
Term
1 Mood Stabilizers that causes weight gain
Definition
Lithium
Term
4 Antidepressants that cause weight gain
Definition
MAO inhibitors,
Mirtazapine,
SSRIs,
Tricyclics,
Term
1 Antihistamine causing weight gain
Definition
1st generation
Cettirizine
Term
4 Antihypertensives causing weight gain
Definition
α1 blockers,
Clonidine,
Methyldopa,
Minoxidil
Term
5 Antipsychotics causing weight gain
Definition
Chlorpromazine
Clozapine
Olanzapine
Quetiapine
Thioridazine
Term
3 Hormones causing weight gain
Definition
Corticosteroids,
Medroxyprogesterone,
Megestrol
Term
4 Hypoglycemics causing weight gain
Definition
Insulin,
Meglitinides,
Sulfonyureas,
thiazolidinediones
Term
What occurs when the following drugs are taken, and what occurs when they are d/c: Amphetamine and other sympathomimetic appetite suppressants
Sibutramine (Meridia)
Orlistat (Xenical)?
Definition
FDA-Approved Prescription Drugs-Anorectic agents – suppress appetite: Once these drugs are stopped weight is usually regained
Term
What is the reported mean weight loss for 44-54 weeks of sibutramine?
Definition
4.45 kg compared to placebo
Term
Trials examining effect of d/c sibutramine noted what weight regain?
Definition
43-55%
Term
The following adverse effects are associated w/what drug: tolerance with continued use, physical dependence, hypertension, tachycardia, insomnia, agitation?
Definition
Methamphetamine (C-II)/Sympathomimetic Agents
Term
Besides methamphetamine (C-II), what are 3 other sympathomimetic agents with similar properties and restrictions
Definition
Phentermine (Adipex-P, lonamin) C-IV,
Diethylpropion (Tenuate) C-IV,
Phendimetrazine (Bontril) C-III
Term
What is the MOA of Sibutramine (Meridia) C-IV?
Definition
MOA: Serotonin and norepinephrine reuptake inhibitor;
Similar to venlafaxine (Effexor), an antidepressant
Term
For what use is Sibutramine (Meridia) C-IV indicated?
Definition
Indicated for weight loss in obese patients in conjunction with a reduced-calorie diet and appropriate exercise
Term
The following are adverse effects of what drug: constipation, nausea, headache, insomnia, dry mouth?
Definition
Sibutramine (Meridia) C-IV
Term
What is the MOA of orlistat?
Definition
MOA: reversible inhibitor of lipase enzymes in stomach and small intestine – fat absorption reduced by 30%
Term
For what use is Orlistat (Xenical) indicated?
Definition
Indicated for weight loss in obese patients in conjunction with a reduced-calorie diet and appropriate exercise
Term
How must diet be modified w/Orlistat (Xenical)?
Definition
Minimal absorption of drug. To be effective must be taken with reduced calorie diet with *no more than 30% in fat calories*
Term
The following adverse effects related to reduced fat absorption are associated w/what drug: oily spotting, flatulence, fecal urgency, and fatty stool. *Also fat soluble vitamin deficiency (A,D,E,K)*?
Definition
Orlistat (Xenical)
Term
What are 2 drug interactions associated w/Orlistat (Xenical)?
Definition
Drug interactions: warfarin (elevated INR), cyclosporine (decreased absorption)
Term
What supplements must be taken w/Orlistat (Xenical)?
Definition
Supplement: take multivitamin 2 hrs before or after Xenical to replace fat soluble vitamins. psyllium w/ea dose may reduce gi ade
Term
What is the dose and cost for orlistat: xenical vs. ali?
Definition
xenical: 120 mg w/meals containing fat adn $260/mo; alli: 60 mg w/meals containing fat and $70/mo
Term
How much did orlistat pts lose w/orlistat vs placebo?
Definition
2.9 kg
Term
What Prescription Drugs Being Used “Off-Label” for Weight Loss is the Drug of choice for overweight diabetes patients because of either no weight gain or some modest weight loss?
Definition
Metformin (Glucophage)
Term
What Prescription Drugs Being Used “Off-Label” for Weight Loss is a First line hypoglycemic agent for Type 2 diabetes?
Definition
Metformin (Glucophage)
Term
What Prescription Drugs Being Used “Off-Label” for Weight Loss is an Antidepressant and smoking cessation agent?
Definition
Bupropion (Wellbutrin, Zyban)
Term
What Prescription Drugs Being Used “Off-Label” for Weight Loss Demonstrated weight loss in several RDBPC trials using 300-400mg per day over 6 months?
Definition
Bupropion (Wellbutrin, Zyban)
Term
What Prescription Drugs Being Used “Off-Label” for Weight Loss is an Antiepileptic agent with serotonergic and dopaminergic effects?
Definition
Zonisamide (Zonegran)
Term
What Prescription Drugs Being Used “Off-Label” for Weight Loss demonstrated Short term weight loss seen in epileptic trials compared to placebo with
Adverse effects similar to topiramate, plus is sulfa drug?
Definition
Zonisamide (Zonegran)
Term
What Prescription Drugs Being Used “Off-Label” for Weight Loss is an Antiepileptic agent, with
Weight loss potentially due to GI adverse effects such as nausea and taste aversion?
Definition
Topiramate (Topamax)
Term
What Prescription Drugs Being Used “Off-Label” for Weight Loss Also causes paresthesias, ataxia, kidney stones, metabolic acidosis? Cost?
Definition
Topiramate (Topamax) cost is $50/mo
Term
What Prescription Drugs Being Used “Off-Label” for Weight Loss is an Antiepileptic agent that is
Considered weight neutral but some reports of weight loss?
Definition
Levetiracetam (Keppra)
Term
What Prescription Drugs Being Used “Off-Label” for Weight Loss has effects Most likely due to anorexia? What is the cost?
Definition
Levetiracetam (Keppra). $200/mo
Term
What Prescription Drugs Being Used “Off-Label” for Weight Loss is Being offered in weight loss clinics, pushed on infomercials with
No evidence for weight loss in scientific literature?
Definition
Human chorionic gonadotropin (HCG)
Term
What Prescription Drugs Being Used “Off-Label” for Weight Loss is the First of new class of drugs for diabetes called incretin mimetics?
Definition
Exenatide (Byetta)
Term
What Prescription Drugs Being Used “Off-Label” for Weight Loss is a Synthetic version of molecule isolated from Gila monster saliva?
Definition
Exenatide (Byetta)
Term
What Prescription Drugs Being Used “Off-Label” for Weight Loss Stimulates GLP-1 receptors to release insulin from pancreas and slow stomach emptying time?
Definition
Exenatide (Byetta)
Term
What Prescription Drugs Being Used “Off-Label” for Weight Loss had Weight loss observed in diabetic trials, in particular with metformin?
Definition
Exenatide (Byetta)
Term
What Prescription Drugs Being Used “Off-Label” for Weight Loss shows Common adverse effects that include nausea and vomiting and comes in a
Daily SC injection at a cost of @230 per autoinject pen?
Definition
Exenatide (Byetta)
Term
What Prescription Drugs Being Used “Off-Label” for Weight Loss is a Synthetic amylin analog for diabetics already requiring insulin?
Definition
Pramlintide (Symlin)
Term
What Prescription Drugs Being Used “Off-Label” for Weight Loss is dosed 240 mcg SC TID and is associated with 3.7% weight loss in 204 non-insulin using obese patients (mean BMI = 38) over 10 weeks?
Definition
Pramlintide (Symlin)
Term
What are 3 weight loss drugs that have been taken off the market?
Definition
Dexfenfluramine (Redux),
Fenfluramine (Pondimin)
Both were the “Fen” in Phen-Fen (Phen = phentermine),
Phenylpropanolamine (Dexatrim)
Term
What are 2 weight loss drugs that have been taken off the market b/c they were associated w/valvular heart disease?
Definition
Dexfenfluramine (Redux),
Fenfluramine (Pondimin)
Both were the “Fen” in Phen-Fen (Phen = phentermine) serotonin release and reuptake inhibitors
Term
What weight loss drug has been taken off the market b/c it Increased risk of hemorrhagic stroke seen in patients using PPA in dietary supplements?
Definition
Phenylpropanolamine (Dexatrim)
Term
What are 3 natural weight loss products Marketed as thermogenic (‘fat-burning’) agents that the fda has limited regulatory control over b/c they are dietary supplements? What are their active ingredients?
Definition
Ma-huang (ephedra) – contains ephedrine and PPA;
Mixed acting adrenergic agonist,
Bitter orange – contains synephrine (sympathomimetic);
Causes drug interactions similar to grapefruit juice,
Country mallow or heartleaf – contains ephedra
Term
What natural weight loss dietary supplement Causes drug interactions similar to grapefruit juice (cyp3a4 enzymes in gut)?
Definition
Bitter orange – contains synephrine (sympathomimetic); common replacement for ephedra
Term
What is an Experimental Drug for Weight Loss?
Definition
Rimonabant (Acomplia in Europe)
Term
What weight loss drug has the following adverse effects: compared to placebo, doubles the rate of psychiatric effects such as depression, mood disorder, anxiety, and insomnia (seems to block pleasure as well as cravings)?
Definition
Rimonabant (Acomplia in Europe)
Term
What weight loss drug is being Studied for both weight loss and smoking cessation
Also has decreased waist circumference and triglyceride levels, and increased HDL cholesterol levels?
Definition
Rimonabant (Acomplia in Europe)
Term
How much was spent on prescription diet drugs vs. herbal and supplemental diet drugs?
Definition
$459 million vs. $20 billion on herbal supplement/diet drugs
Term
What is the #1 diet weight loss drug in the country, found in guarana, green tea extract, yerba mate, kola nut, and trimethylxanthine?
Definition
caffeine
Term
What natural product is theorized to inhibit production of lipis but clinical trail in JAMA showed no effect on weight?
Definition
garcinia
Term
In what class do the following MOA of agents for weight loss fall: adrenergic, serotonergic, incretin mimetics, amylin analogs, cannabinoid receptor antagonists, leptin analogues?
Definition
anorexiant
Term
In what class do the following MOA of agents for weight loss fall: decrease fat absorption, metformin-like?
Definition
metabolic
Term
In what class do the following MOA of agents for weight loss fall: phosphodiesterase inhibitors, b3-receptor agonists, thyroid stimulants?
Definition
thermogenic
Term
What are 4 FDA-approved anorexiant drugs w/short-term use?
Definition
methamphetamine (schedule II), phendimetrazine (schedule III), diethylpropion (schedule IV), phentermine (schedule IV)
Term
What is the only FDA-approved anorexiant drugs w/long-term use?
Definition
sibutramine (schedule IV)
Term
For what use was sibutramine (meridia) originally developed?
Definition
antidepressant
Term
What weight loss drug is metabolized by cyp3a4 enzyme to active metabolites which are then eliminated by kidneys?
Definition
sibutramine (meridia)
Term
What are contraindications/precautions of sibutramine (meridia)?
Definition
hx of poorly controlled/uncontrolled htn, cad, arrhythmia, stroke. precautions: renal impairment, depression.
Term
Is orlistat approved for long or short term use?
Definition
long-term
Term
What was the best result for trials of sibutramine for weight loss?
Definition
sibutramine plus lifestyle modification: 12.1 kg
Term
For how long did randomized orlistat or placebo plus lifestyle changes trials last?
Definition
4 yrs: 800 kcal/day deficit diet
Term
The following are ade of antidiabetic agent: gi cramping, potential for lactic acidosis w/high plasma levels?
Definition
metformin (glucophage)
Term
What off-label use of antidiabetic agents for weight loss has the following ade: n/v, hypoglycemia?
Definition
pramlintide
Term
What is the cost for pramlintide (symlin)?
Definition
cost $260 for 2 autoinject pens
Term
What drug is contraindicated if hx of *sulfa allergy*? What is the cost?
Definition
zonisamide (zonegran; cost $80/mo)
Term
What is the MOA of bupropion?
Definition
inhibits reuptake of norepinephrine and dopamine
Term
What drugs theoretically should have anorexiant effect by increasing synaptic serotonin levels w/short-term weight loss apparent but tolerance develops quickly after several mos?
Definition
SSRI
Term
What off-label use of misc agents for weight loss involves popular use in weight loss clinics w/no evidence for weight loss in scientific literature?
Definition
HCG and B12
Term
What off-label use of misc agents for weight loss promotes fat loss in GH-deficient children w/no evidence of efficacy in obese individuals that may increase insulin resistance?
Definition
rHGH- recombinant human growth hormone
Term
What are the risks of ephedra-containing dietary supplements such as ephedra, ma-huang, and country mallow?
Definition
increased risk of stroke, mi, seizure, and death in particular w/higher doses or in combo w/caffeine
Term
How does the fda get dietary supplements off the market?
Definition
must *prove* they cause harm to get them OFF the market
Term
How are most natural products marketed?
Definition
*thermogenic* or "fat-burning agents"
Term
What other natural product may reduce glucose and lipid levels but not weight?
Definition
chromium
Term
What other natural product does not convert to testosterone like dhea but may increase thyroid levels?
Definition
7-keto-dhea
Term
What is the moa of caffeine?
Definition
inhibits phosphodiesterase leading to increased levels of intracellular c-AMP
Term
What are the pharmacokinetics for caffeine?
Definition
metabolized by cyp 1a2 w/ t1/2 = 3-5hrs
Term
What are ade of caffeine?
Definition
dose-related: insomnia, restlessness, irritability, anxiety, tachycardia, extra systoles, mild diuresis; severe: seizures, arrythmias
Term
What are drug interactions for caffeine?
Definition
drugs that induce (nicoteine, aeds) or inhibit (*cipro*, cimetidine) cyp1a2 enzymes
Term
What is a south african plant made famous by 60 minutes episode w/no clinical efficacy trials- concerns about hepatotoxicity, contaminated products?
Definition
hoodia gordonii
Term
What drug is a Selective inhibitor of CB1 endocannabinoid receptor that was
Studied for both weight loss and smoking cessation and
Also has decreased waist circumference and triglyceride levels, and increased HDL cholesterol levels?
Definition
rimonabant (accomplia in europe)
Term
What drug has the following ade: compared to placebo, doubles the rate of psychiatric effects such as depression, mood disorder, anxiety, and insomnia (seems to block pleasure as well as cravings)?
Definition
rimonabant (accomplia in europe)
Term
What experimental drug for weight loss involves a hormone secreted by fat cells that inhibits feeding and increases energy expenditure?
Definition
metroleptin
Term
What experimental drug for weight loss shows obese individuals that appear resistant to agent as monotherapy?
Definition
metroleptin
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