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2 Pharm Unit > Drugs Test 2 > Flashcards

Drugs Test 2 Flashcards

1
Q

Morphine

A

-Opioid agonist
-Mu receptor
-
-
-sedate, constipate, resp depress, nausea/vomit
-euphoria, miosis
-Analgesia

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2
Q

Hydromorphone

A
  • Mu Opioid analgesics
  • Faster onset and more potent than morphine
  • analgesia
    [mnemonic] (put in brackets)
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3
Q

hydrocodone

A
  • Mu Opioid analgesics
  • metabolized to hydromorphone by CYP2D6
  • analgesia
    [mnemonic] (put in brackets)
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4
Q

oxycodone

A
  • Mu Opioid analgesics
  • metabolized to oxymorphone by CYP2D6
  • analgesia
    [mnemonic] (put in brackets)
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5
Q

oxymorphone

A
  • Mu Opioid analgesics
  • analgesia
    [mnemonic] (put in brackets)
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6
Q

codeine

A
  • Mu Opioid analgesics
  • CYP2D6 pharmacogenetic variability is clinically significant
  • converted to morphine by demethylation
  • analgesia
    [mnemonic] (put in brackets)
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7
Q

heroin

A
  • Mu Opioid analgesics
  • converted to monoacetyl morphine and morphine in the brain,
    rapid onset pharmacokinetics
  • analgesia
    [mnemonic] (put in brackets)
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8
Q

methadone

A
  • Mu Opioid analgesics
  • oral, long acting half life of 15-60 hours
  • analgesia, maintenance for opioid drug addiction
    [mnemonic] (put in brackets)
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9
Q

meperidine

A
  • Mu Opioid analgesics
  • prolonged half life in patients with renal failure due to decreased elimination
  • faster onset and less potency than morphine, converted in liver
    to nor-meperidine (CNS stimulation, convulsions)
  • can produce serotonin syndrome, esp. when combined with SSRIs or MAOIs
  • analgesia
    [mnemonic] (put in brackets)
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10
Q

tramadol

A
  • Mixed agonists, antagonists
  • partial mu agonist activity and monoamine reuptake inhibitor activity
  • metabolized by CYP2D6 and CYP3A4; CYP2D6 produces the active metabolite
  • for mild to moderate acute and chronic pain
    [mnemonic] (put in brackets)
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11
Q

tapentadol

A
  • Mixed agonists, antagonists
  • partial mu agonist activity and monoamine reuptake inhibitor activity
  • less pharmacogenetic variability than tramadol, greater mu receptor efficacy
  • metabolized mainly by CYP2C9, CYP2C19, and a little by CYP2D6
  • for mild to moderate acute and chronic pain
    [mnemonic] (put in brackets)
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12
Q

pentazocrine

A
  • Mixed agonists, antagonists
  • kappa receptor agonists and mu receptor partial agonist, antagonist
  • for acute, short term pain
    [mnemonic] (put in brackets)
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13
Q

nalbuphen

A
  • Mixed agonists, antagonists
  • kappa receptor agonists and mu receptor partial agonist, antagonist
  • for acute, short term pain
    [mnemonic] (put in brackets)
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14
Q

buprenorphine

A
  • Mixed agonists, antagonists
  • kappa receptor agonists and mu receptor partial agonist
  • high affinity for mu receptor, difficult to reverse its mu agonist effect
  • for acute, short term pain, useful for drug abuse and addiction
    [mnemonic] (put in brackets)
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15
Q

Diphenoxylate

A
  • antidiarrheal opioids
  • poorly absorbed or not absorbed after oral administration
  • diarrhea
    [mnemonic] (put in brackets)
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16
Q

loperimide

A
  • antidiarrheal opioids
  • poorly absorbed or not absorbed after oral administration
  • diarrhea
    [mnemonic] (put in brackets)
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17
Q

naloxone

A
  • opioid antagonists
  • bind to opioid receptors and antagonize effects of opioid agonists
  • parenteral administration
  • antagonize opiate effects
    [mnemonic] (put in brackets)
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18
Q

naltrexone

A
  • opioid antagonists
  • bind to opioid receptors and antagonize effects of opioid agonists
  • oral administration
  • antagonize opiate effects
    [mnemonic] (put in brackets)
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19
Q

alvimopan

A
  • opioid antagonists
  • bind to opioid receptors and antagonize effects of opioid agonists
  • poorly absorbed or not absorbed after oral administration
  • prevent GI side effects of opioids
    [mnemonic] (put in brackets)
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20
Q

methylnatrexone

A
  • opioid antagonists
  • bind to opioid receptors and antagonize effects of opioid agonists
  • quaternary ammonium derivative
  • IV peripherally restricted antagonist
  • constipation
    [mnemonic] (put in brackets)
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21
Q

morphine-naltrexone

A
  • abuse resistent opioids
  • extended release morphine with sequestered naltrexone
  • Provide pain relief but prevent or reduce opioid abuse
    [mnemonic] (put in brackets)
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22
Q

oxycodone naltrexone

A
  • abuse resistent opioids
  • oxycodone with naltrexone
  • Provide pain relief but prevent or reduce opioid abuse
    [mnemonic] (put in brackets)
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23
Q

chlorpromazine

A

-Typical antipsychotic (phenothiazine)
-DA antag (more D2 than D1), also M, alpha-adrenergic, and H1 receptor antag
-piperazine side chains, high potency, 4-8 week delay in onset of action, metabolized by CYP2D6 & CYP3A4 for elimin
-
-neuroleptic malignant syndrome, striatal D block: Parkisonian effects, dystonias, akathisia; D receptor upregulation: tardive dyskinesias; block L-DOPA effects; at high doses: some tolerance, hypotension, hyper/hypothermia, seizures, coma, ventricular tachycardia; increased prolactin release (less prominent)
-M block: hyperthermia, tachycardia, urinary retention, memory impairment, blurred vision, constipation, and confusion; alpha-adrenergic block: vasodilation, orthostatic hypotension and light-headedness, reflex tachycardia, and sexual dysfuntion; H1 block: sedation & weight gain
-Antipsychotic

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24
Q

fluphenazine

A

-Typical antipsychotic (phenothiazine)
-DA antag (more D2 than D1)
-piperazine side chains, high potency, 4-8 week delay in onset of action, metabolized by CYP2D6 & CYP3A4 for elimin; fluphenazine decanoate-slow release formula, deep gluteal IM injection, for non-compliant patients
-
-neuroleptic malignant syndrome, striatal D block: Parkisonian effects, dystonias, akathisia; D receptor upregulation: tardive dyskinesias; block L-DOPA effects; at high doses: some tolerance, hypotension, hyper/hypothermia, seizures, coma, ventricular tachycardia; increased prolactin release (less prominent)
-
-antipsychotic

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25
Q

thiothixene

A

-Typical antipsychotic (thioxanthene)
-DA antag (more D2 than D1)
-medium potency, 4-8 week delay in onset of action, metabolized by CYP2D6 & CYP3A4 for elimin
-
-neuroleptic malignant syndrome, striatal D block: Parkisonian effects, dystonias, akathisia; D receptor upregulation: tardive dyskinesias; block L-DOPA effects; at high doses: some tolerance, hypotension, hyper/hypothermia, seizures, coma, ventricular tachycardia; increased prolactin release (less prominent)
-
-antipsychotic

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26
Q

haloperidol

A

-Typical antipsychotic (butyrophenone)
-DA antag (more D2 than D1)
-high potency, 4-8 week delay in onset of action, metabolized by CYP2D6 & CYP3A4 for elimin; haloperidol decanoate-slow release formula, deep gluteal IM injection, for non-compliant patients
-
-neuroleptic malignant syndrome, striatal D block: Parkisonian effects, dystonias, akathisia; D receptor upregulation: tardive dyskinesias; block L-DOPA effects; at high doses: some tolerance, hypotension, hyper/hypothermia, seizures, coma, ventricular tachycardia; increased prolactin release (less prominent)
-prominent prolactin release
-antipsychotic

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27
Q

aripiprazole

A
  • Atypical antipsychotic
  • competitive partial DA2 ag, 5HT2A antag; also alpha-adrenergic & H1 antag
  • metabolized by CYP2D6 & CYP3A4 for elimin (inhib of CYP2D6 & CYP3A4 -> decr elimination; induction of CYP3A4 -> incr elimination)
  • discontinue gradually to avoid withdrawal/relapse
  • minimal increase in prolactin release, sedation & weight gain (5-HT block); potentiation of CNS depressant effects
  • alpha-adren block: vasodilation, orthostatic hypotension & light-headedness, reflex tachycardia, and sexual dysfunction; H1 block: sedation & weight gain
  • antipsychotic
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28
Q

clozapine

A

-Atypical antipsychotic
-DA2 antag, 5HT2A antag; also M, alpha-adrenergic, & H1 antag
-metabolized by CYP1A2, CYP2D6, & CYP3A4 for elimin (inhib of CYP2D6 & CYP3A4 -> decr elimination; induction of CYP1A2 & CYP3A4 -> incr elimination)
-
-minimal increase in prolactin release, sedation & weight gain (5-HT block); potentiation of CNS depressant effects
-M block: hyperthermia, tachycardia, urinary retention, memory impairment, blurred vision, constipation, confusion; alpha-adren block: vasodilation, orthostatic hypotension & light-headedness, reflex tachycardia, and sexual dysfunction; H1 block: sedation & weight gain; incr risk weight gain & metabolic effects (glucose intol, lipid abnormal, incr risk DM-type2, cardiovascular disease); incr risk agranulocytosis & leukopenia
-antipsychotic

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29
Q

olanzapine

A

-Atypical antipsychotic
-DA2 antag, 5HT2A antag; also M, alpha-adrenergic, & H1 antag
-metabolized by CYP1A2, CYP2D6, & CYP3A4 for elimin (inhib of CYP2D6 & CYP3A4 -> decr elimination; induction of CYP1A2 & CYP3A4 -> incr elimination)
-
-minimal increase in prolactin release, sedation & weight gain (5-HT block); potentiation of CNS depressant effects
-severe metabolic: major weight gain and glucose, cholesterol, and TGs increase; M block: hyperthermia, tachycardia, urinary retention, memory impairment, blurred vision, constipation, confusion; alpha-adren block: vasodilation, orthostatic hypotension & light-headedness, reflex tachycardia, and sexual dysfunction; H1 block: sedation & weight gain; incr risk weight gain & metabolic effects (glucose intol, lipid abnormal, incr risk DM-type2, cardiovascular disease)
-antipsychotic, bipolar

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30
Q

paliperidone

A

-Atypical antipsychotic
-DA2 antag, 5HT2A antag
-metabolized by CYP2D6 & CYP3A4 for elimin(inhib of CYP2D6 & CYP3A4 -> decr elimination - less extent than others in class)
-
-minimal increase in prolactin release, sedation & weight gain (5-HT block); potentiation of CNS depressant effects
-incr risk weight gain & metabolic effects (glucose intol, lipid abnormal, incr risk DM-type2, cardiovascular disease)
-antipsychotic

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31
Q

quetiapine

A

-Atypical antipsychotic
-DA2 antag, 5HT2A antag; also M, alpha-adrenergic, & H1 antag
-metabolized by CYP2D6 & CYP3A4 for elimin (inhib of CYP2D6 & CYP3A4 -> decr elimination; induction of CYP3A4 -> incr elimination)
-
-minimal increase in prolactin release, sedation & weight gain (5-HT block); potentiation of CNS depressant effects
-M block: hyperthermia, tachycardia, urinary retention, memory impairment, blurred vision, constipation, confusion; alpha-adren block: vasodilation, orthostatic hypotension & light-headedness, reflex tachycardia, and sexual dysfunction; H1 block: sedation & weight gain; incr risk weight gain & metabolic effects (glucose intol, lipid abnormal, incr risk DM-type2, cardiovascular disease)
-antipsychotic, bipolar

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32
Q

risperidone

A

-Atypical antipsychotic
-DA2 antag, 5HT2A antag
-major active metabolite is paliperidone, partially metabolized by CYP2D6 for elimination; risperidone microspheres (slow release IM formula for noncompliant patients)
-
-minimal increase in prolactin release, sedation & weight gain (5-HT block); potentiation of CNS depressant effects
-incr risk weight gain & metabolic effects (glucose intol, lipid abnormal, incr risk DM-type2, cardiovascular disease)
-antipsychotic, bipolar

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33
Q

prochlorperazine

A

-Anti-emetic, bit antipsychotic
-H1 antag, mild DA2 antag
-
-
-
-anti-emetic

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34
Q

promethazine

A

-Anti-emetic, bit antipsychotic
-H1 antag, mild DA2 antag
-
-
-
-anti-emetic

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35
Q

Diazepam

A

-Benzodiezapine
-Bind GABA-A receptors, enhance channel open frequency
-Antianxiety without sedation at low dose
- Long half life
-
-
-Anti-anxiety, withdrawal, muscle relaxant

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36
Q

Chlordiazepoxide

A

-Benzodiezapine
-Bind GABA-A receptors, enhance channel open frequency
-Antianxiety without sedation at low dose
-
-
-
-Anti-anxiety

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37
Q

Alprazolam

A

-Benzodiezapine
-Bind GABA-A receptors, enhance channel open frequency
-Antianxiety without sedation at low dose
-Short half life
-
-
-Anti-anxiety, insomnia

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38
Q

Oxazepam

A

-Benzodiezapine
-Bind GABA-A receptors, enhance channel open frequency
-Antianxiety without sedation at low dose
-
-
-
-Anti-anxiety

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39
Q

Lorazepam

A

-Benzodiezapine
-Bind GABA-A receptors, enhance channel open frequency
-Antianxiety without sedation at low dose
-Intermediate half life
-
-
-Anti-anxiety, insomnia

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40
Q

Midazolam

A

-Benzodiezapine
-Bind GABA-A receptors, enhance channel open frequency
-Antianxiety without sedation at low dose
-Ultrashort half life
-
-
-Preanesthetic medication

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41
Q

Flumenazil

A

-Benzodiezapine Antagonist
-Competitive binding at BZ binding site on GABA-A
-
-IV admin, multiple doses because short half life
-
-
-Reverse BZ induced respiratory depression

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42
Q

Zolpidem

A

-Non-Benzodiezepine
-Bind at BZ binding site on GABA-A
-
-Enhance GABA mediated GABA channel opening
-IV admin resulted in cardiovascular and respiratory depress.
-
-Induce Sleep

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43
Q

Zaleplon

A

-Non-Benzodiezepine
-Bind at BZ binding site on GABA-A
-
-Enhance GABA mediated GABA channel opening
-IV admin resulted in cardiovascular and respiratory depress.
-
-Induce Sleep

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44
Q

Pentobarbital

A

-Barbiturates
-Bind to barbiturate binding site on GABA-A, increase channel open time
-
-Can open channel in the absence of GABA, marked CYP induction, short/intermediate half life
-Respiratory and cardiovascular depression, drowsiness, confusion, diminished motor skills, impaired judgement
-
-Preoperative sedation

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45
Q

Phenobarbital

A

-Barbiturates
-Bind to barbiturate binding site on GABA-A, increase channel open time
-
-Can open channel in the absence of GABA, marked CYP induction, Long half life
-Respiratory and cardiovascular depression, drowsiness, confusion, diminished motor skills, impaired judgement
-
-Anticonvulsant

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46
Q

Amobarbital

A

-Barbiturates
-Bind to barbiturate binding site on GABA-A, increase channel open time
-
-Can open channel in the absence of GABA, marked CYP induction, ultrashort half life
-Respiratory and cardiovascular depression, drowsiness, confusion, diminished motor skills, impaired judgement
-
-Preoperative sedation

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47
Q

Thiopental

A

-Barbiturates
-Bind to barbiturate binding site on GABA-A, increase channel open time
-
-Can open channel in the absence of GABA, marked CYP induction, ultrashort half life
-Respiratory and cardiovascular depression, drowsiness, confusion, diminished motor skills, impaired judgement
-
-Anesthesia induction

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48
Q

Buspirone

A

-Serotonin Antagonist
-Partial 5HT-1A receptor blocker
-
-Anxiolytic effects, no CNS depression
-
-
-Anxiolytic

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49
Q

Propranolol

A 
-Beta blocker 
-
-
-
-
-
-Blocks palpitations, shaking, sweating, stage fright
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50
Q

carbamazepine

A
  • antiepileptic
  • Inhibit voltage-activated Na+ channels and thus prolong
    the refractory period and reduce sustained firing
  • Induces P-450s, increases its own metabolism and metab. of other antiepileptics
    during chronic administration
  • ## Oral, slow absorption, highly lipid soluble and good CNS penetration, metabolized by P-450s
  • Hepatotoxicity, teratogenic effects
    -Partial simple and complex and Tonic Clonic seizures, trigeminal neuralgia, bipolar disorder
    [mnemonic] (put in brackets)
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51
Q

ethosuximide

A
  • antiepileptic
  • ## Inhibit voltage-activated Ca2+ channels and thus inhibit rhythmic activity in thalamic neurons
  • well absorbed orally, no plasma protein binding, long half life (30-60 hours)
    75% is metabolized by liver P450s, 25% excreted unchanged in urine
    -
    -
  • Absence seizures
    [mnemonic] (put in brackets)
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52
Q

gabapentin

A
  • antiepileptic
  • ## Blocks Ca channels and release of glutamate, enhances GABAergic synaptic transmission
  • Not metabolized and does not induce hepatic enzymes, not bound to plasma proteins,
    short half life, eliminated by kidney
    -
    -
  • simple or complex partial, tonic-clonic seizures
    [mnemonic] (put in brackets)
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53
Q

lamotrigine

A
  • antiepileptic
  • Inhibit voltage-activated Na+ channels and thus prolong
    the refractory period and reduce sustained firing
    Inhibits release of glutamate
  • Drug interactions: half life is decreased by enyzyme inducing drugs (eg carbam. and Phenyt.)
    and is increased by valproic acid
  • ## Drug is metabolized by liver-
  • simple or complex partial, tonic-clonic seizures, bipolar
    [mnemonic] (put in brackets)
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54
Q

phenobarbital

A
  • antiepileptic
  • ## Enhance inhibitory GABAergic neurotransmission
  • ## well absorbed orally, freely penetrates brain,75% inactivated in hepatic microsomal system
  • teratogenic effects
  • Simple partial, recurrent tonic-clonic, and febrile seizures
    [mnemonic] (put in brackets)
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55
Q

phenytoin

A
  • antiepileptic
  • Mainly blocks voltage gated Na+ channels, also blocks Ca2+ channels
  • oral absorption is slow, but distribution is rapid and brain concentrations are high
  • Oral for chronic treatment, IV for emergency; high plasma protein binding
    drug interaction: Enhances P-450 system and increases metabolism of doxycycline and cyclosporine
    -
  • gingival hyperplasia, megaloblastic anemia, teratogenic effects
  • partial simple, partial complex and tonic-clonic seizures, emergency treatment of status epilepticus
    [mnemonic] (put in brackets)
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56
Q

valproic acid

A
  • antiepileptic
  • Inhibit voltage-activated Na+ channels and thus prolong
    the refractory period and reduce sustained firing;
    Inhibit voltage-activated Ca2+ channels and thus inhibit rhythmic activity;
    Enhance inhibitory GABAergic neurotransmission
    -
  • ## orally effective, rapidly absorbed, 90% plasma protein binding, metabolized by liver P450s
  • hepatotoxicity, thrombocytopenia, teratogenic effects
  • myoclonic seizures, second line treatment for tonic-clonic and absence seizures, bipolar
    [mnemonic] (put in brackets)
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57
Q

pregabalin

A
  • antiepileptic
  • ## blocks Na channels and release of glutamate-
    -
  • Thrombocytopenia
  • simple and complex partial seizures
    [mnemonic] (put in brackets)
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58
Q

topiramate

A
  • antiepileptic
  • ## blocks Na channels and increases activity of postsynaptic GABA receptors-
    -
    -
  • Simple and complex partial, tonic-clonic seizures
    [mnemonic] (put in brackets)
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59
Q

levetiracetam

A
  • antiepileptic
  • ## modifies glutamate and GABA release via binding to synaptic protein SV2A-
    -
    -
  • Adjunctive treatment of simple and complex partial and tonic-clonic seizures
    [mnemonic] (put in brackets)
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60
Q

clonazepam

A
  • benzodiazepine
  • ## Enhance inhibitory GABAergic neurotransmission
  • ## tolerance develops after 1-6 months-
  • myoclonic and absence seizures
    [mnemonic] (put in brackets)
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61
Q

diazepam

A
  • benzodiazepines
  • ## Enhance inhibitory GABAergic neurotransmission
  • ## tolerance develops after 1-6 months-
  • Status epilepticus
    [mnemonic] (put in brackets)
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62
Q

lorazepam

A 
benzodiazepines
- Enhance inhibitory GABAergic neurotransmission
-
- tolerance develops 1-6 months
-
-
- Status epilepticus
[mnemonic] (put in brackets)
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63
Q

Levodopa (L-DOPA)

A
  • DA synthesis enhancers
  • dopamine precurser
  • Anorexia, hypotension, arrythmias
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64
Q

L-DOPA + carbidopa

A

-DA synthesis enhancers

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65
Q

Entacapone

A
  • DA synthesis enhancers
  • COMT inhibitor
  • dyskinesia, confusion, hypotension
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66
Q

Amantadine

A

-DA synthesis enhancers
-increases DA release, blocks cholinergic and
NMDA receptors.
-Should not be given to patients with CHF and glaucoma.

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67
Q

Apomorphine

A
  • Dopamine receptor agonists

- Used for acute “off periods” in parkinsons patients.

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68
Q

bromocriptine

A

-Dopamine receptor agonists
-D2 agonist, D1 partial agonist
-Depression, confusion, GI problems, arrythmias
(DO not give to patients with heart or mental problems.

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69
Q

pramipexole

A

-Dopamine receptor agonists
-D2 and D3 agonist
-Depression, confusion, GI problems, arrythmias
(DO not give to patients with heart or mental problems.

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70
Q

ropinirole

A

-Dopamine receptor agonists
-D2 and D3 agonists
-Depression, confusion, GI problems, arrythmias
(DO not give to patients with heart or mental problems.

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71
Q

benztropine

A
  • anticholinergics
  • Muscarinic antagonist
  • typical antimuscarinic effects
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72
Q

trihexyphenidyl

A
  • anticholinergics
  • Muscarinic antagonist
  • typical antimuscarinic effects
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73
Q

rasagiline

A
  • MAO b inhibitors

- Not oxidized to amphetamines

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74
Q

selegiline

A
  • MAO b inhibitors

- metabolized to methamphetamine and amphetamines

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75
Q

donepezil

A

-ACh inhibitors

Tremors, bradycardia, nausia, vomiting, diarrhea

76
Q

galantamine

A
  • ACh inhibitors

- Tremors, bradycardia, nausia, vomiting, diarrhea

77
Q

rivastigmine

A
  • ACh inhibitors

- Tremors, bradycardia, nausia, vomiting, diarrhea

78
Q

tacrine

A
  • ACh inhibitors
  • Tremors, bradycardia, nausia, vomiting, diarrhea
  • Hepatotoxicity
79
Q

memantine

A
  • NMDA antagonist
  • Blocks NMDA receptor preventing large calcium influx within the cell.
  • Dizziness, confusion, constipation
80
Q

acetazolamide

A

-carbonic anhydase inhibitor
-NaHCO3 gets left in the urine
-
-
-allergy, ammonia exacerbates hepatic encephalopathy, bone marrow suppression, paresthesias
-metabolic acidosis, kidney stones
-open angle glaucoma, altitude sickness, counter metab. alkalosis from diuretics

81
Q

glycerin

A

-osmotic agent
-Draw water into blood, increase urine production
-Oral administration
-
-Hyponatremia, hyponatremia w/ dehydration
-May cause hyperglycemia after its metabolism
-Acute renal failure, acute tubular necrosis, dialysis disequilibrium, reduce intraoccular pressure for glaucoma

82
Q

mannitol

A

-osmotic agent
-Draw water into blood, increase urine production
-
-IV use only
-Hyponatremia, hyponatremia w/ dehydration
-
-Acute renal failure, acute tubular necrosis, dialysis disequilibrium, reduce intraoccular pressure for glaucoma, reduce brain swelling for neurosurgery

83
Q

bumetanide

A

-loop agents
-Inhibit Na+/K+, 2Cl- symporter in thick ascending limb
-Enter the urine via organic anion transporter in proximal tubule
-Short halflife (0.8 hrs)requires frequent dosing, Works only if in the lumen, not subject to tubuloglomerular feedback
-Hyponatremia, hypokalemia, volume depletion, metabolic alkalosis, hyperurecemia
-
-Pulmonary edema, congestive HF, Hypertension, Nephrotic syndrome, Edema and ascites of cirrhosis, chronic renal failure

84
Q

ethacrynic acid

A
  • loop agents
  • Inhibit Na+/K+, 2Cl- symporter in thick ascending limb
  • Enter the urine via organic anion transporter in proximal tubule
  • Short halflife (1.0 hrs)requires frequent dosing, Works only if in the lumen, not subject to tubuloglomerular feedback
  • Hyponatremia, hypokalemia, volume depletion, metabolic alkalosis, hyperurecemia
  • Ototoxicity
  • Pulmonary edema, congestive HF, Hypertension, Nephrotic syndrome, Edema and ascites of cirrhosis, chronic renal failure
85
Q

furosemide

A
  • loop agents
  • Inhibit Na+/K+, 2Cl- symporter in thick ascending limb, weak carbonic anhydrase inhibitor
  • Enter the urine via organic anion transporter in proximal tubule
  • Short halflife (1.5 hrs)requires frequent dosing, Works only if in the lumen, not subject to tubuloglomerular feedback
  • Hyponatremia, hypokalemia, volume depletion, metabolic alkalosis, hyperurecemia
  • Sulfa allergy
  • Pulmonary edema, congestive HF, Hypertension, Nephrotic syndrome, Edema and ascites of cirrhosis, chronic renal failure
86
Q

torsemide

A

-loop agents
-Inhibit Na+/K+, 2Cl- symporter in thick ascending limb
-Enter the urine via organic anion transporter in proximal tubule
-Short halflife (3.5 hrs)requires frequent dosing, Works only if in the lumen, not subject to tubuloglomerular feedback
-Hyponatremia, hypokalemia, volume depletion, metabolic alkalosis, hyperurecemia
-
-Pulmonary edema, congestive HF, Hypertension, Nephrotic syndrome, Edema and ascites of cirrhosis, chronic renal failure

87
Q

chlorothiazide

A

-thiazide
-Block Na/Cl symporter in DCT, secondary carbonic anhydrase inhibiton activity
-
-Enter urine via organic ion transporter in proximal tubule, calcium sparing, doesn’t disrupt medullary gradient
-Hypotension, hypokalemia, hyponatremia, metabolic alkalosis, hypercalcemia, hyperuricemia
-Small risk of sudden death or renal cell carcinoma, sulfonilamide allergy
-Hypertension, Edema from CHF, calcium nephrolithiasis, osteoporosis, nephrogenic diabetes insipidus

88
Q

hydrochlorothiazide

A

-thiazide
-Block Na/Cl symporter in DCT, secondary carbonic anhydrase inhibiton activity
-
-Enter urine via organic ion transporter in proximal tubule, calcium sparing, doesn’t disrupt medullary gradient
-Hypotension, hypokalemia, hyponatremia, metabolic alkalosis, hypercalcemia, hyperuricemia
-Small risk of sudden death or renal cell carcinoma, sulfonilamide allergy
-Acute diuresis with edema, Hypertension, Edema from CHF, calcium nephrolithiasis, osteoporosis, nephrogenic diabetes insipidus

89
Q

metolazone

A
  • thiazide-like
  • Block Na/Cl symporter in DCT
  • LOOOOONG half-life (20 hrs)
  • Enter urine via organic ion transporter in proximal tubule, calcium sparing, doesn’t disrupt medullary gradient
  • Hypotension, hypokalemia, hyponatremia, metabolic alkalosis, hypercalcemia, hyperuricemia
  • Small risk of sudden death or renal cell carcinoma, sulfonilamide allergy
  • Hypertension, Edema from CHF, calcium nephrolithiasis, osteoporosis, nephrogenic diabetes insipidus
90
Q

Amiloride

A

-K+ Sparing Diuretic
-ENaC blocker (distal convoluted & collecting duct)
-
-21 hr half life. NSAIDS decrease efficiency.
-CNS, GI
-hyperkalemia (esp in AIDS)
-adjunct w/ thiazide or loop diruetic to reduce K loss. Edema, heart failure, LIDDLE’s syndrome. aerosol for cystic fibrosis. Also acts as an ANTI-DIURETIC for: Lithium-induced diabetes insipidus (blocks lithium uptake by Na channels)

91
Q

Triamterene

A

-K+ Sparing Diuretic
-ENaC blocker (distal convoluted & collecting duct), folate antagonist
-
-4 hr half life. NSAIDS decrease efficiency.
-CNS, GI
-hyperkalemia (esp in AIDS), megaloblastic anemia in cirrhosis
-adjunct w/ thiazide or loop diruetic to reduce K loss. Edema, heart failure, LIDDLE’s syndrome. aerosol for cystic fibrosis.

92
Q

Spironolactone

A

-
-NSAIDS decrease efficiency.
-diarrhea, gastritis, gastric bleeding, CNS, rash
-hyperkalemia, anti-androgen (feminization), anti-progesterone (menstrual prob), malignancies
-primary hyperaldosteronism, ascites & edema from cirrhosis! Adjunct w/ thiazide or loop diuretic.

93
Q

Eplerenone

A

-
-clearance down by CYP3A4 inhibitors. NSAIDS decrease efficiency.
-diarrhea, gastritis, gastric bleeding, CNS, rash
-hyperkalemia, anti-androgen (feminization), anti-progesterone (menstrual prob)
-Adjunct w/ thiazide or loop diuretic.

94
Q

Chlorpropamide

A

-Antidiuretic
-up ADH secretion
-
-
-
-
-

95
Q

Desmopressin

A

-Antidiuretic
-V2 agonist (bit of V1)
-
-
-water intoxication
-coronary artery constriction
-Central Diabetes insipidus

96
Q

Vasopressin

A

-Antidiuretic
-V1 & V2 agonist
-
-
-water intoxication
-coronary artery constriction
-desmopressin is better, but: Central Diabetes insipidus

97
Q

Probenecid

A

-Uricosuric
-inhibit OAT (organic anion transporter)
-
-biphasic effect on gout
-kidney stones
-inhibits excretion of MANY drugs (including diuretics)
-gout

98
Q

Allopurinol

A
  • Misc (Anti-Gout)
  • ## inhibit xanthine oxidase-
    -
    -
    -gout
99
Q

Colchicine

A
  • Misc (Anti-Gout / Anti-inflammatory)
    -reduces neutrophil activity (painful inflammation)
    -
    -
    -
    -
    -gout
100
Q

cyclophosphamide

A

-DNA alkylating agents (bischoloroethyl amines)
-dechlor. makes electrophile attacks nucleophile in DNA base
-nitrogen analog of mustard gas
-less reactive, must be activated in liver/tumor tissues
-
-anti-tumor

101
Q

mechlorethamine

A

-DNA alkylating agents (bischoloroethyl amines)
-dechlor. makes electrophile attacks nucleophile in DNA base
-nitrogen analog of mustard gas
-Highly reactive
-
-anti-tumor

102
Q

nitrosureas

A 
-alkylating agents
-
-
-cross BBB, little cross reactivity w/ other alkylators
-
-brain tumors
103
Q

procarbazine

A 
-alkylating agents (other)
-
-
-little x-react w/ other antineo. MOPP reg., metab. to alkylate
-leukemogenic 5-10%
-Hodgkin's in the MOPP regimen
104
Q

cisplatin

A

-platinum coordination complexes
-cross link DNA, inhibit DNA biosynthesis
-
-cell cycle non specific
-nephro toxic, acoustic nerve dysfunction [no myelosupression]
-ovarian and testicular cancer

105
Q

methotrexate

A

-anti-tumor antimetabolites
-dihydrofolate reductase inh., blocks DNA syn., RNA precursor, blocks thymidylate formation
-folic acid analog, accumulates as polyglutamate
-S-phase specific, [folinic acid is antidote for rescue, leucovorin]
-
-anti-tumor

106
Q

leucovorin

A

-anti-tumor antimetabolites (folinic acid rescue)
-replaces FH4 in thymidylate synthetase cycle
-formyl-FH4
-
-
-rescue to methotrecate

107
Q

5-fluorouracil

A

-anti-tumor antimetabolites, pyrimidine antagonist
-metabolite FdUMP direct inh. thymidylate sythetase, incorp. into DNA/RNA
-Flourine on 5 carbin 5-FU
-S-phase
-
-anti-tumor

108
Q

capecitabine

A

-anti-tumor antimetabolites, pyrimidine antagonist
- metabolized to 5FU, FdUMP direct inh. thymidylate synthetase
-
-oral prodrug of 5-FU, pref. activ. in tumor tissue
-
-colon cancer, refractory breast cancer

109
Q

cytosine arabinoside (cytarabine, ara C)

A

-anti-tumor antimetabolites, pyrimidine antagonist
-araC–>araCMP—>araCTP inh. DNA synthesis, high rates DNA breaks
-
-activation requires deoxycytidine
-
-anti-tumor

110
Q

6-mercaptopurine

A
  • anti-tumor antimetabolites, purine antagonist
  • metabolite inhib. purine synthesis, xDNA, xRNA –>fraud base incorporation
  • thiol derivative on purine
  • s-phase, activ. by HGPRT, inactiv. by xanthine oxidase, low bioav. w/ milk
  • must decrease dose when allopurinol use
  • anti-tumor
111
Q

6-thioguanine

A

-anti-tumor antimetabolites, purine antagonist
-metabolite inhib. purine synthesis, xDNA, xRNA –>fraud base incorporation
-thiol derivative on purine, guanine
-s-phase,activated by HGPRT
-
-anti-tumor

112
Q

bleomycin

A
  • anti-tumor antibiotics
  • DNA strand scission
  • natural
  • small doses at first!
  • anaphylaxis, pulmonary fibrosis [no myelosuppression]
  • broad spectrum of tumors, combination regimens
113
Q

daunorubicin

A

-anti-tumor antibiotics, topoisomerase inhibitors
-DNA intercalation, topo II binding, DNA scission
-
-
-irreversible cardiac toxicity
-anti-tumor

114
Q

doxorubicin

A

-anti-tumor antibiotics, topoisomerase inhibitors
-DNA intercalation, topo II binding, DNA scission
-
-
-irreversible cardiac toxicity
-anti-tumor

115
Q

paclitaxel

A

-mitotic spindle poisons
-enhances tubulin polymerization (blocks disassembly)
-plant alkaloid
-
-
-ovarian and advanced breast cancers

116
Q

vinblastine

A

-mitotic spindle poisons (vinca alkaloids)
-inhibit tubulin polymerization
-
-M-phase
-myelosuppression(limits dose), nausea
-hodgkin and lymphomas(AVBD regimen)

117
Q

vincristine

A

-mitotic spindle poisons (vinca alkaloids)
-binds to microtubules
-
-
-mild non-dose limiting supression, significant neurotoxicity
-child leukemia, Hodkins MOPP regimen (o=oncovi=vincristine)

118
Q

irinotecan

A

-topoisomerase inhibitors (camptothecins)
-bind topo/dna complex, block religation, also double strand break
-
-s phase for replication blocking double strand
-severe diarrhea
-colorectal cancer

119
Q

topotecan

A

-topoisomerase inhibitors (camptothecins)
-bind topo/dna complex, block religation, also double strand break
-
-s phase for replication blocking double strands
-myelosupression
-ovarian and lung cancer

120
Q

daunorubicin

A

-anti-tumor antibiotics, topoisomerase inhibitors

121
Q

doxorubicin

A

-anti-tumor antibiotics, topoisomerase inhibitors

122
Q

etoposide

A

-topoisomerase inhibitors
-ternary complex with topo II, scission, block religation of double strand
-
-s phase
-
-

123
Q

tamoxifen

A

-antagonist of hormone action(estrogen)
-competitive inhibitor of estrogen binding to ER (SERM)
-
-partial agonist
-hot flashes, blood clots, increased risk of uterine cancer
-female and male breast, uterine endometrium

124
Q

raloxifene

A

-antagonist of hormone action (SERM)
-SERM
-
-partial agonist
-
-prevent breast cancer in osteoporosis women

125
Q

anastrozole

A

-antagonist of hormone action (aromatase inhibitor)
-inhibit androgen to estrogen conversion
-
-post menopause not pre menopause
-joint pain, loss of bone density
-ER+ breast cancer, especially tamoxifen resistant

126
Q

letrozole

A

-antagonist of hormone action (aromatase inhibitor)
-inhibit androgen to estrogen conversion
-
-post menopause not pre menopause
-joint pain, loss of bone density
-ER+ breast cancer, especially tamoxifen resistant

127
Q

exemestane

A

-antagonist of hormone action (aromatase inhibitor)
-inhibit androgen to estrogen conversion
-
-post menopause not pre menopause
-joint pain, loss of bone density
-ER+ breast cancer, great reducer of high risk postmenopause!

128
Q

leuprolide

A

-antagonist of hormone action-(anti-androgen)
-GnRH-R agonist
-synthetic analog of GnRH
-pulsatile-elevates levels, cont. high doses greatly lowers levels(castration)
-
-prostate cancer

129
Q

flutamide

A

-antagonist of hormone action
-androgen recetor antagonis
-
-ineffective alone due to rapid receptor mutation
-
-prostate cancer, must use with leuprolide

130
Q

prednisone

A

-adrenocorticosteroids
-induce apoptosis in leukemia cells
-
-
-
-multi drug reg. (MOPP) leukemia, lymphoma, myeloma. Palliative in other cancers

131
Q

lapatinib

A

-“Targeted” agents (EGFR kinase inhibitors)

132
Q

erlotinib

A

-“Targeted” agents (EGFR kinase inhibitors)
-EGF receptor protein tyrosine kinase inhibitor
-
-
-
-non small cell lung cancer (brain head and neck trials)

133
Q

lapatinib

A

-“Targeted” agents (HER2 kinase inhibitor)
-small protein HER 2 kinase inhibitor
-
-
-
-breast cancer

134
Q

imatinib

A

-“Targeted” agents (bcr/abl kinase inhibitor)
-small molecule inhibitor of abl protein tyrosine kinase
-
-
-
-chronic myelogenous leukemia

135
Q

cetuximab

A

-“Targeted” agents (chimeric/humanized antibodies)
-chimeric EGFR antibody
-
-
-
-
-colon cancer, head and neck cancer

136
Q

trastuzumab

A

-“Targeted” agents (chimeric/humanized antibodies)
-HER2 antibody, immune system mediated effects
-humanized antibody
-
-
-refractory metastatic breast cancer

137
Q

brentuximab vedotin

A

-“Targeted” agents (chimeric/humanized antibodies)
-IgG binds CD30 surface antigen, vedotin enters & mitotic spindle poison
-chimeric IgG conjugated vedotin
-
-
-some Hodgkin and non-hodgkin lymphoma(anaplastic large cell)

138
Q

desflurane

A

-Volatile general anesthetics
-inhib in CNS at GABA & glycine receptors & reduce glutamate transmission
-blood-gas part coef=0.42; metabolized at 0.02%; produces prompt recovery
-
-malignant hyperthermia; respiratory depression; decreased arterial BP (decr. HR, CO, & syst vascular res)
-airway irritation, minimal myocardial depression
-anesthesia maintenance

139
Q

isoflurane

A

-Volatile general anesthetics
-inhib in CNS at GABA & glycine receptors & reduce glutamate transmission
-blood-gas part coef=1.4; 0.2% metabolized
-
-malignant hyperthermia; respiratory depression; decreased arterial BP (decr. HR, CO, & syst vascular res)
-airway irritation, minimal myocardial depression
-anesthesia maintenance

140
Q

nitrous oxide

A

-Volatile general anesthetics
-inhib in CNS at GABA & glycine receptors & reduce glutamate transmission
-blood-gas part coef=0.46; very insoluble
-
-malignant hyperthermia; respiratory depression; decreased arterial BP (decr. HR, CO, & syst vascular res)
-little side effects
-adjunct to potent volatile anesthetics

141
Q

sevoflurane

A

-Volatile general anesthetics
-inhib in CNS at GABA & glycine receptors & reduce glutamate transmission
-blood-gas part coef=0.68; metabolized at 2-5%; produces prompt recovery
-
-malignant hyperthermia; respiratory depression; decreased arterial BP (decr. HR, CO, & syst vascular res)
-no airway irritation; minimal myocardial depression
-anesthesia maintenance

142
Q

dantrolene

A 
-
-
-
-
-
-
-Treats malignant hyperthermia
143
Q

succinylcholine

A

-N2 non-competitive depolarizing inhibitor
-agonist for Na channel and keeps it open
-
-hydrolysis from plasma ChE nor AChE!, short DOA
-K–>cardiac arrest, contraction of eye muscles
-can cause malignant hypothermia
-relax muscles during surgery/vent

144
Q

etomidate

A 
-
-
-
-
-
-
-
145
Q

ketamine

A 
-
-
-
-
-
-
-
146
Q

methohexital

A 
-
-
-
-
-
-
-
147
Q

propofol

A 
-
-
-
-
-
-
-
148
Q

thiopental

A 
-
-
-
-
-
-
-
149
Q

alfentanil

A 
-
-
-
-
-
-
-
150
Q

fentanyl

A 
-
-
-
-
-
-
-
151
Q

remifentanil

A 
-
-
-
-
-
-
-
152
Q

sufentanil

A 
-
-
-
-
-
-
-
153
Q

flumazenil

A 
-
-
-
-
-
-
-
154
Q

midazolam

A 
-
-
-
-
-
-
-
155
Q

benzocaine

A

-Local Anesthetics- Esters
-Binds intracell. portion of voltage-gated Na channels blocks depolarization
-
-Topical ester
-Numb tongue,lighthead,convulse/uncon,coma,resp arrest,cardiac tox.
-methemoglobeniemia, rare allergic response
-nerve block to eliminate sensory and motor response to stimulus

156
Q

cocaine

A

-Local Anesthetics- Esters
-Binds intracell. portion of voltage-gated Na channels blocks depolarization
-
-topical ester
-Numb tongue,lighthead,convulse/uncon,coma,resp arrest,cardiac tox.
-Vasoconstriction!, MI, Seizures
-nerve block to eliminate sensory and motor response to stimulus

157
Q

procaine

A

-Local anesthetic-Ester
-Binds intracell. portion of voltage-gated Na channels blocks depolarization
-
-45-60min, lowest potency and hydrophobicity
-Numb tongue,lighthead,convulse/uncon,coma,resp arrest,cardiac tox.
-rare allergic response
-nerve block to eliminate sensory and motor response to stimulus

158
Q

tetracaine

A

-local anesthetic-ester
-Binds intracell. portion of voltage-gated Na channels blocks depolarization
-
-plasm esterase metab. 60-180min (longest ester), highest potency
-Numb tongue,lighthead,convulse/uncon,coma,resp arrest,cardiac tox.
-rare allergic response
-nerve block to eliminate sensory and motor response to stimulus

159
Q

bupivicaine

A

-Local Anesthetics-Amides
-Binds intracell. portion of voltage-gated Na channels blocks depolarization
-
-240-480min (longest), highest potency
-Numb tongue,lighthead,convulse/uncon,coma,resp arrest,cardiac tox.
-
-nerve block to eliminate sensory and motor response to stimulus

160
Q

lidocaine

A

-Local anesthetic- amide
-Binds intracell. portion of voltage-gated Na channels blocks depolarization
-tertiary amine
-liver metab. 60-120, intermediate potency, TOPICAL or SubQ
-Numb tongue,lighthead,convulse/uncon,coma,resp arrest,cardiac tox.
-
-nerve block to eliminate sensory and motor response to stimulus

161
Q

mepivacaine

A

-Local Anesthetics-Amides
-Binds intracell. portion of voltage-gated Na channels blocks depolarization
-
-90-180 min, intermediate potency
-Numb tongue,lighthead,convulse/uncon,coma,resp arrest,cardiac tox.
-
-nerve block to eliminate sensory and motor response to stimulus

162
Q

prilocaine

A

-Local Anesthetics-Amides
-Binds intracell. portion of voltage-gated Na channels blocks depolarization
-
-60-120min
-Numb tongue,lighthead,convulse/uncon,coma,resp arrest,cardiac tox.
-
-nerve block to eliminate sensory and motor response to stimulus

163
Q

ropivacaine

A
  • Local Anesthetics-Amides
  • Binds intracell. portion of voltage-gated Na channels blocks depolarization
  • S-isomer of the racemic mixture
  • 180-360min (2nd longest amide)
  • Numb tongue,lighthead,convulse/uncon,coma,resp arrest,cardiac tox.
  • Less toxicity with similar potency to RACEMIC BUPIVICAINE
  • nerve block to eliminate sensory and motor response to stimulus
164
Q

amitriptyline

A
  • tricyclics (TCA’s)
  • block ser & NE reuptake
  • block histamine, muscarinic, adrenergic R’s.
  • 2 weeks to work, long half-life, kidney elim & bit hepatic microsomes
  • antimuscarinic, sedation (H1 R), sex down, weight up, delirium, tachycardia
  • seizures, slowing A-V conductance, orthostatic hypotension (alpha 1 R)
  • Antidepressant
165
Q

amoxapine

A
  • tricyclics (TCA’s)
  • block ser & NE reuptake
  • block histamine, muscarinic, adrenergic R’s.
  • 2 weeks to work, long half-life, kidney elim & bit hepatic microsomes
  • antimuscarinic, sedation (H1 R), sex down, weight up, delirium, tachycardia
  • seizures, slowing A-V conductance, orthostatic hypotension (alpha 1 R)
  • Antidepressant
166
Q

imipramine

A
  • tricyclics (TCA’s)
  • block ser & NE reuptake
  • block histamine, muscarinic, adrenergic R’s.
  • 2 weeks to work, long half-life, kidney elim & bit hepatic microsomes
  • antimuscarinic, sedation (H1 R), sex down, weight up, delirium, tachycardia
  • seizures, slowing A-V conductance, orthostatic hypotension (alpha 1 R)
  • Antidepressant
167
Q

nortriptyline

A
  • tricyclics (TCA’s)
  • block ser & NE reuptake
  • block histamine, muscarinic, adrenergic R’s.
  • 2 weeks to work, long half-life, kidney elim & bit hepatic microsomes
  • antimuscarinic, sedation (H1 R), sex down, weight up, delirium, tachycardia
  • seizures, slowing A-V conductance, orthostatic hypotension (alpha 1 R)
  • Antidepressant
168
Q

citalopram

A
  • SSRI’s
  • block ser reuptake
  • neurogenesis in hippocampus (via BDNF)
  • 2 wks to work, kidney elim, block P450, high first-pass effect, binds plasma proteins
  • nausea, anxiety, insomnia… late: sex down
  • late: anorexia, mania
  • Antidepressant
169
Q

escitalopram

A
  • SSRI’s
  • block ser reuptake
  • neurogenesis in hippocampus (via BDNF)
  • 2 wks to work, kidney elim, block P450, high first-pass effect, binds plasma proteins
  • nausea, anxiety, insomnia… late: sex down
  • late: anorexia, mania
  • Antidepressant
170
Q

fluoxetine

A
  • SSRI’s
  • block ser reuptake
  • neurogenesis in hippocampus (via BDNF)
  • demethylated to active. 2 wks to work, kidney elim, block P450, high first-pass effect, binds plasma proteins
  • nausea, anxiety, insomnia… late: sex down
  • late: anorexia, mania
  • Antidepressant, bipolar
171
Q

sertraline

A
  • SSRI’s
  • block ser reuptake
  • neurogenesis in hippocampus (via BDNF)
  • 2 wks to work, kidney elim, block P450, high first-pass effect, binds plasma proteins
  • nausea, anxiety, insomnia… late: sex down
  • late: anorexia, mania
  • Antidepressant
172
Q

duloxetine

A

-SNRI’s
-block ser, NE reuptake (but UNRELATED to TCA’s)
-
-1/4 bound to plasma proteins, elim mostly kidney. metab by CYP1A2, CYP2D6
-nausea, anxiety, insomnia, sex down [same as SSRI’s!]
-high dose up blood pressure
-depression refractory to SSRI’s

173
Q

venlafaxine

A

-SNRI’s
-block ser, NE reuptake (but UNRELATED to TCA’s)
-
-mostly bound to plasma proteins, elim mostly kidney. metab by CYP2D6
-nausea, anxiety, insomnia, sex down [same as SSRI’s!]
-high dose up blood pressure
-depression refractory to SSRI’s

174
Q

bupropion

A

-atypicals
-inhibit dopamine reuptake
-often combined w/ TCA’s
-
-nausea, insomnia, nervous, headache
-tinnitus
-rapid-cycling bipolar, depression

175
Q

mirtazapine

A

-atypicals
-blocks alpha2 R’s. (down Ser, NE)
-often combined w/ TCA’s
-
-nausea, insomnia, nervous, headache
-tinnitus
-rapid-cycling bipolar, depression

176
Q

nefazodone

A

-atypicals
-inhibit reuptake of 5HT & blocks 5HT2 R’s
-often combined w/ TCA’s
-
-nausea, insomnia, nervous, headache
-tinnitus
-rapid-cycling bipolar, depression

177
Q

phenelzine

A

-MAOi’s
-3rd-line after SSRI’s & TCA’s
-inhibit MAO-A & B
-
-orthostatic hypotension, tachycardia, agitated, pyschoses
-serotonin syndrome, cheese effect
-depression

178
Q

selegiline

A

-MAOi’s
-3rd-line after SSRI’s & TCA’s
-inhibit MAO-B (and A @ high conc)
-
-orthostatic hypotension, tachycardia, agitated, pyschoses
-serotonin syndrome, cheese effect
-depression

179
Q

tranylcypromine

A

-MAOi’s
-3rd-line after SSRI’s & TCA’s
-inhibit MAO-A & B
-
-orthostatic hypotension, tachycardia, agitated, pyschoses
-serotonin syndrome, cheese effect
-depression

180
Q

lithium

A
  • bipolar treatment
  • unclear. block hyrolysis of IP to inositol, blocks GSK-3B, inhibits 5HT1A & 1B, enhances glutamate reuptake
  • onset takes 3-4 wks, substitutes for Na (adverse!).
  • Low therapeutic index! kidney elim. 20 hr half-life.
  • tremors, confusion, teratogenic, down thyroid, diabetes insipidus
  • arrhythmias, coma, convulsions
  • bipolar
181
Q

amphetamine

A
  • Stimulants

- this drug not specifically described in lecture, just know it’s same as other amphetamine stimulants

182
Q

atomoxetine

A

-Stimulants but “not stimulant”
-NE reuptake inhibitor
-NOT habit-forming
-
-
-
-ADHD

183
Q

dextro-amphetamine

A

-Stimulants
-Up pre-synaptic cytoplasmic DA, NE release from vesicles. inhibit MAO. Thus DA, NE released into cleft by vesicles & non-vesicles.
-
-Full GI aborption, liver metab, urine excrete
-euphoria, insomnia, anxiety, vertigo, confusion, nausea, hypertension, diarrhea
-arrhythmias, addiction
-narcolepsy, ADHD

184
Q

methylphenidate

A

-high conc. to brain
-Full GI aborption, liver metab, urine excrete (as ritalinic acid)
-euphoria, insomnia, anxiety, vertigo, confusion, nausea, hypertension, diarrhea
-arrhythmias, addiction
-narcolepsy, ADHD

185
Q

modafinil

A

-Stimulants
-unclear
-
-euphoria, insomnia, anxiety, vertigo, confusion, nausea, hypertension, diarrhea
-arrhythmias, addiction
-Fewer psycho, euphoric, & cognition effects!
-narcolepsy

2 Pharm Unit (17 decks)

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