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504 Pharm > Exam 2 > Flashcards

Exam 2 Flashcards

1
Q

Methadone (Dolophine)

A

Strong opioid agonist
Orally effective
Longer duration of action
Used for detoxification and controlled withdrawal from heroin and morphine

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2
Q

Codeine

A

Moderate opioid agonist
Metabolized to morphine for analgesic activity
Used with aspirin and acetaminophen for moderate pain
Included in many cough syrups for relief of cough
0.5% concentration in opium

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3
Q

Pentazocine (Talwin)

A

Mixed opioid agonist-antagonist
A kappa-receptor agonist with weak mu-receptor antagonist activity
Orally administered for treating moderate to severe pain
Parenteral formulation as a preanesthetic medication
Precipitates a withdrawal syndrome in a morphine abuser

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4
Q

Buprenorphine (Buprenex)

A

Mixed opioid agonist-antagonist
A partial agonist at mu-receptors and an antagonist at kappa-receptors
Resistant to naloxone reversal
Used to manage cocaine addiction and heroin abuse

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5
Q

Naloxone(Narcan)

A

Opioid antagonist
A competitive antagonist (half life time is 1-2 hours)
No obvious effects in normal people
Antagonist-precipitated withdrawal
Intravenous injection for treating opioid overdose

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6
Q

Naltrexone (ReVia)

A 
Opioid antagonist
A competitive antagonist (half life time is 10 hours)
Antagonist-precipitated withdrawal
A "maintenance" drug for addicts
Also used in treatment of alcoholics
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7
Q

Carbamazepine (Tegratol)

A

Enhance Na+ channel inactivation
P450 inducer (1/2 life shortens from 36 hr to 8-12 hr with chronic treatment)
Common adverse reactions: diplopia, ataxia, drowsiness
Tegratol-XR sustained release form
Used also for neuropathic pain, bipolar disorder
Induces metabolism of other drugs

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8
Q

Topiramate (Topomax)

A

A D-fructose analog
Multiple mechanisms of action: blocks Na channels, increases affinity of GABA for its receptors, blocks AMPA-type glutamine receptors
1/2 time = 21 hr; mostly excreted unchanged in urine
Broad spectrum anticonvulsant, widely used
Common adverse reactions: sleepiness, dizziness, balance issues, often resolve over time
Also used for migraine prophylaxis

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9
Q

Ethosuximide (Zarontin)

A 
Block Ca channels
Drug of choice for absence epilepsy 
T-type Ca channels not involved in transmitter release
No plasma protein binding
1/2 life 40-60 hrs with renal excretion
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10
Q

Valproate (Depakote)

A

Enhance GABAergic inhibition
Broad spectrum anticonvulsant
Divalproex Na is a sustained release form
Hepatotoxicity - contraindicated in hepatic disease and children less than 2 yrs
Mixed mechanism: also blocks Na channels
Also used for bipolar disorder and migraine prophylaxis
Inhibits metabolism of other drugs and is highly protein bound

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11
Q

Levetiracetam (Keppra)

A

Mechanism of action: SV2A target

Most common type of seizure affected: partial complex

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12
Q

Tiagabine (Gabitril)

A

Mechanism of action: potentials GABAergic inhibition

Most common type of seizure affected: partial complex

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13
Q

Clozapine (Clozaril)

A

Parkinson’s disease therapy #1: replace the lost dopamine (L-DOPA, cabidopa)
D2 antagonist active on mesolimbic dopamine receptors, can blunt psychotic effects such as hallucinations, delirium, depression, sleep disturbances

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14
Q

Bromocryptine (Parlodel)

A 
Parkinson's disease therapy #2:
Directly activate dopamine receptors in striatum
Prototype, a D2 agonist 
Greater than 90% 1st pass metabolism
3 hour 1/2 life
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15
Q

Cabergoline (off label)

A

Parkinson’s disease therapy #2:
Directly activate dopamine receptors in striatum
Has 66 hr 1/2 life
2x/week PO

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16
Q

Ropinirole (Requip)

A

Parkinson’s disease therapy #2:
Directly activate dopamine receptors in striatum
Causes fewer dyskinesias than L-DOPA
Often used intitially, or in combo with L-DOPA
Adverse effects: nausea, mental confusion, hallucinations

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17
Q

Selegiline (Eldepryl)

A

Parkinson’s disease therapy #3:
Scavenge free radicals and inhibit MAO-B
Prototype

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18
Q

Tetrabenazine (Xenazine)

A

Huntington’s disease
Approved in 2008: VMAT2 inhibitor that depletes dopamine; reduces dyskinesias but not cognitive seizing or mood issues
Might also be useful for tardive dyskinesias

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19
Q

Lidocaine

A

Amide
The most broadly used local anesthetic
Intermediate duration (approx 2 hr spinal, 30-60 min for topical or infiltration)
Higher systemic toxicity than ester-linked drugs
Metabolized by liver
Uses: spinal, epidural, local, topical
Careful: concurrent use with amiodarone

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20
Q

Procaine (Novocaine)

A 
Ester
Introduced in 1905
Short acting (40 sec plasma 1/2 life)
Low toxicity
Main use: infiltration and regional anes
Interaction: PABA blocks sulfonamide action
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21
Q

Tetracaine (Pontocaine)

A

Ester
Intermediate duration of action (slowly hydrolyzed: 2 hr spinal anes, 30-60 min for topical)
Higher systemic toxicity than other esters
Tends to cause mucous membrane irritation, uticaria, burning
Main uses: spinal & topical anes of nose and throat for diagnostic procedures

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22
Q

Bupivacaine (Marcaine)

A

Amide
Widely used local anesthetic
Long duration of action (3-9 hr regional anes, plasma 1/2 life 3.5 hr adult, >8 hr neonate)
Concurrent epidural use with opiates in labor can reduce the amount of opiate needed for analgesia
More cardiac effects than lidocaine due to slower dissociation from cardiac Na channels
Synergistic with anti-arrhythmics on heart - can induce arrhythmias (treatment: iv admin of lipid emulsions)

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23
Q

Morphine

A

Strong opioid agonist
4-6 hour duration of action
Active metabolite: morphine-6- glucuronide
Treatment of severe pain associated with trauma, myocardial infarction, and cancer
Major active ingredient in opium (10%)

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24
Q

Hydrocortisone/cortisol

A

Glucocorticoid
Endogenous
Short acting, weaker
Corticosteroid for treatment of Addison’s disease

25
Prednisone and prednisolone
Synthetic glucocorticoid | Intermediate in level of anti-inflammation and salt retaining activity
26
Dexamethasone and betamethasone
Synthetic glucocorticoid Long acting Maximal anti-inflammatory and minimal salt retaining activity
27
Fludrocortisone
Synthetic mineralocorticoid Most widely used Longer half life. Good to use for patents with adrenal insufficiency Adverse effects: salt retention and HTN
28
Aminoglutethimide
Inhibitor of adrenal corticoid steroids Inhibits the conversion of cholesterol to pregnenolone Used for patients with adrenal and/or pituitary adenoma
29
Spironolactone
Inhibitor of adrenal corticoid steroids Antagonist for mineralocorticoid receptor Uses: aldosteronism, such as adrenal adenoma
30
Mifepristone (RU486)
Inhibitor of adrenal corticoid steroids Antagonist for glucocorticoid receptor Also acts as an antagonist for progesterone receptor = medical abortion
31
Levothyroxine (Synthroid)
Drug of choice for hypothyroidism for hormonal replacement therapy T4 that is converted in body to T3
32
Liothyronine (L-T3)
Used for acute/severe hypothyroidism (myxedema coma) | Direct T3, don't have to convert
33
Hyperthyroidism drugs
A: Thioureylene - drugs of choice Propylthiouracil (PTU) Methimazole (Tapazol) Used for control of symptoms prior to surgery B. Iodide or KI (Lugol's) Used for thyroid storm, preop thyroidectomy C. Radioactive iodide Severe hyperthyroidism combo w/ Synthroid D. Beta blockers Propranolol For life threatening crisis thyroid storm
34
Estrogens and Progestins
E: ethinyl estradiol and mestranol P: ester of progesterone and 19-nortestosterone
35
Clomiphene (Clomid)
Fertility drug Estrogen receptor antagonist Inhibits neg feedback = induces ovulation
36
Selective estrogen receptor modulators (SERMs)
Anti cancer drugs Tamoxifen (Nolvadex): estrogen antagonist in breast tissue, inhibits proliferation of breast cancer Raloxifene (Evista): estrogen antagonist in breast and uterin, agonist in bone = prevent post menopausal osteoporosis Femara (Letrozole): aromatase inhibitor, reduces estrogen production
37
Diazepam (Valium)
Long acting benzo with active metabolites | Useful for treatment of sleep disorders associated with anxiety due to a steady state drug concentration
38
Triazolam (Halcium)
Short acting benzo Good for treating sleep disorders in the absence of anxiety Rapid sleep onset with no daytime hangover
39
Zolpidem (Ambien)
Non-benzodiazepine benzodiazepine receptor agonist (NBRAs) | Relatively selective for type 1 benzo receptor. Useful for acute treatment of sleep disorders
40
Eszopiclone (Lunesta)
Non-benzodiazepine benzodiazepine receptor agonist (NBRAs) | Indicated for chronic treatment of insomnia. Rapid onset, longer half life than zolpidem
41
Buspirone (BuSpar)
Anxioselective drug | Useful for treatment of chronic anxiety disorder
42
Treatment of alcoholism
Disulfram (Antabuse): causes you to get sick if you drink, I bite of aldehyde dehydrogenase Acamprosate (Campral): reduces glutamate neurotransmission - refuses relapse in detoxified patients
43
Chlorpromazine (Thorazine)
Typical antipsychotic drug
44
Haloperidol (Haldol)
Typical antipsychotic drug
45
Clozapine (Clozaril)
Atypical antipsychotic drug
46
Aripiprazol (Abilify)
Dopamine system stabilizer (DSS) Atypical antipsychotic drug Stabilizes dopamine in an intermediate state with minor side effects
47
Imipramine (Tofranil)
Trycyclic antidepressant Must be taken chronically, patient compliance problems Side effects can include tachycardia and arrhythmias
48
Fluoxetine (Prozac)
Selective serotonin reuptake inhibitor | Fewer cardiovascular problems
49
Monoamine oxidase inhibitors
Hydrazines: Phenelzine (Nardil) Non-hysrazines: Tranylcypromine (Parnate) Irreversible inhibition of MAO = increased levels of NE, 5HT, and DA.
50
Acetazolamide (Diamox)
Carbonic anhydrase inhibitor | Treats glaucoma, prevent mountain sickness
51
Sucralfate (Carafate)
Protects mucosa from attack by acid and pepsin
52
Cimetidine (Tagament)
Selective H2 receptor antagonist | Blocks acid production from parietal cells
53
Omeprazole (Prilosec)
Proton pump inhibitor Prodrug, activated only at low pH Irreversible, long duration
54
Helicobacter pylori
Antibiotics | Always involves multidrug therapy usually with proton pump inhibitor
55
Tolbutamide (Orinase) | Glyburide (Diabeta)
Oral hypoglycemic agents Sulfonylureas Requires the patient to have functional beta cells = not type 1 Blocks the potassium channel and causes an influx of calcium which releases the insulin
56
Repaglinide (Prandin) | Nateglinide (Starlix)
Oral hypoglycemic agent Meglitinides Similar mechanism to sulfonylurea Less likely to cause hypoglycemia due to short duration of action
57
Metformin (Glucophage)
Antihyperglycemic agent Biguanides Multiple mechanisms that overall inhibits glucose production Does not cause hypoglycemia or increase body weight
58
Acarbose (Precose)
Antihyperglycemic agent Alpha-glucosidase inhibitor Delays carbohydrate absorption Problem of excessive production of gas
59
Rosiglitazone (Avandia) | Pioglitazone (Actos)
Antihyperglycemic agent Thiazolidinediones Should not be used in patients with heart failure

504 Pharm (2 decks)

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