Pharm Exam 3 Flashcards

(189 cards)

1
Q

Cortisol

A

glucocorticoid, secreted in response to ACTH

interact with specific nuclear receptors to increase or decrease the expression of corticoresponsive genes

anti-inflammatory effects largely mediated by transrepression — main mechanism is repression of phospholipase A2; also COX2 & prevents proinflammatory cytokine expression & decreases number of immune cells

metabolic effects: upregulation of trangluconeogenesis enzymes

inactivated by 11βHSD2 (kidneys)

net metabolic effect is increased blood glucose levels

Cushings

A/E: impairs HPA axis, fluid/electrolyte abnormalities, HTN, hyperglycemia, increased risk for infx, osteoporosis/decreased bone density, myopathy, behavioral disturbances, cataracts, retarded growth, fat redistribution, striae

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2
Q

Betamethasone

A

long acting synthetic corticosteroid; anti-inflammatory effects 25x more potent than cortisol; long half life; no Na+ retention effects; 0.25 equivalent dose to cortisol

most commonly used topically for skin infections

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3
Q

Dexamethasone

A

longest acting synthetic corticosteroid; anti-inflammatory effects 25x more potent than cortisol; long half life; no Na+ retention effects; 0.25 equivalent dose to cortisol

used for acute adrenal crisis

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4
Q

Prednisone

A

intermediate strength corticosteroid (12-36 hr duration)

used for acute organ rejection, chronic adrenal insufficiency, rheumatic diseases, giant cell arteritis, systemic skin diseases (atopic dermatitis), IBD,

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5
Q

Triamcinolone

A

intermediate glucocorticoid

used for non-inflammatory joint disease (osteoarthritis), skin diseases (intralesional prep)

also used for asthma

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6
Q

Metyrapone

A

cortisol synthesis inhibitor

inhibits CYP 11B1

used to treat hypercortisolism, diagnostic tests of HPA axis

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7
Q

Ketoconazole

A

cortisol synthesis inhibitor

at high doses, inhibits CYP 17 (to synthesize cortisol & DHEA)
***most effective inhibitor to treat Cushings

anti-fungal at low doses

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8
Q

Aminoglutethimide

A

cortisol synthesis inhibitor

inhibits CYP 11A (initial & rate-limiting step)

used to treat Cushings

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9
Q

Aldosterone

A

endogenous mineralocorticoid

synthesized in response to K+ & angiotensin II

stimulates renal exchange between Na+/K+ or H+

acts on distal tubules & collecting ducts of kidney to increase reabsorption of Na+ (& thus water) & promote K+ excretion — results in fluid retention, increased BP

increase cardiac fibrosis

congenital adrenal hyperplasia commonly caused by CYP 21 mutation — decreases synthesis of aldosterone

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10
Q

Fludrocortisone

A

mineralocorticoid
mineralocorticoid agonist

use with corticosteroid in patients with CAH that also have salt wasting

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11
Q

Alfentanil

A

Opioid (class: Phenylpiperadine)

DOC for outpatient anesthesia — repeated doses do not accumulate, recovery is rapid

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12
Q

Codeine

A

opioid (class phenanthrene)

prodrug that gets metabolized to morphine by CYP 2D6; chemical modification improves 1st pass survivability

potency similar to morphine

oral analgesic & anti-tussive

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13
Q

Fentanyl

A

synthetic opioid (phenylpiperadine class)

80-100x greater potency compared to morphine

shorter duration

highly lipophilic, rapid distribution to other compartments

analgesic; improved cardiac stability; not anesthetic

fentanyl lollipop used for breakthrough pain

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14
Q

Hydrocodone

A

semi-synthetic opioid (class phenanthrene)

greater potency compared to morphine

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15
Q

Meperidine

A

Demerol

synthetic opioid (class phenylpiperadine)

1/10 morphine’s potency

25% bioavailable

used in labor & delivery

reduced likelihood of biliary spasm; does not cause miosis

toxicity: CNS excitation — seizure, tremor, convulsions — metabolite in patients with impaired renal function

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16
Q

Methadone

A
synthetic opioid (class phenylheptanone)
-one of the highest risk 

equipotent with morphine

high bioavailability

once daily dosage, PO

longer acting opioid

improved risk for heroin addicts

some NMDA receptor antagonist properties

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17
Q

Morphine

A

opioid (phenanthrene class)

central effects: analgesia, respiratory depression, anti-tussive (suppresses brainstem cough centers) miosis, tolerance, dependence

peripheral effects: analgesia, constipation, GI spasm; generally increases smooth muscle tone

degranulation of mast cells (which can cause pruritis, systemic hypotension)

active metabolites: excitotoxic, analgesic

main A/E: respiratory depression; also miosis, coma

more effective against continuous, dull pain

opioid for rescue drug for intractable migraine

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18
Q

Oxycodone

A

semi-synthetic opioid (class phenanthrene)

greater potency compared to morphine

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19
Q

Remifentanil

A

synthetic opioid (phenylpiperidine class)

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20
Q

Sufentanil

A

synthetic opioid (phenylpiperidine class)

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21
Q

Tapentadol

A

mixed opioid analgesic

moderate mu receptor agonist, NE reuptake inhibitor

metabolically stable congener of O-desmethyltramadol

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22
Q

Tramadol

A

mixed opioid analgesic — 5HT releaser, NE reuptake inhibitor, weak mu opioid receptor agonist

O-desmethyltramadol metabolite is a stronger mu agonist (CYP2D6 conversion)

toxicity: seziures (NOT respiratory depression)

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23
Q

Naloxone

A

mu opioid antagonist

shortest duration of action, not available orally because it gets destroyed in the liver before getting to bloodstream

use to treat opioid overdose; also alcoholism (by helping remove the positive reinforcement)

in healthy subjects does not alter pain threshold but increases hormone secretion

hyperalgesic in post surgery patients
attenuates/reduces analgesic effects

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24
Q

Naltrexone

A

opioid antagonist

longest duration of action
available orally

addict maintenance

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25
Nalmefene
opioid antagonist intermediate duration of action not available orally
26
Diphenhydramine
1st generation antihistamine - prototype inverse agonist of H1 receptor; works best if administered prior to histamine release; also, competitive antagonist for muscarinic receptors crosses BBB very well, causes significant sedation; significant anti-muscarinic effects (dry mouth, tachycardia, blurred vision, constipation) cleared by CYP2D6 most 1st gen antihistamines are metabolized in the liver & excreted in urine in modified form contraindicated in pregnancy anti-emetic (from anti-muscarinic activity)
27
Promethazine
1st generation H1 blocker significant central anti-cholinergic --sedative & antiemetic cleared by CYP2D6 commonly used for motion sickness, N/V rescue drug for intractable migraine A/E skin rash
28
Doxepin
potent H1 antagonist (1st gen) primarily used as anti-depressant drowsiness & anticholinergic effects
29
Fexofenedine
2nd generation H1 blocker (prototype) with longer duration of action active metabolite of terfenidine without QT prolongation minimal sedative & anti-muscarinic activity (similar to loratadine) most 2nd gen antihistamines are excreted in the urine in unmetabolized form
30
Cetirizine
H1 blocker (2nd gen) poor penetration of BBB; sedation is limited; BUT drowsiness is a serious side effect may have benefit in asthma patients useful in pediatric patients
31
Loratadine
2nd generation H1 blocker oral, relatively non-sedating rapidly absorbed by GI tract, converted to active form by CYP450s--- drug interactions does not readily cross BBB; preferentially binds peripheral receptors long duration of action
32
Desloratadine
2nd generation H1 blocker active metabolite of loratadine more expensive
33
Olopatadine
new anti-histamine on the horizon nasal spray, ophthalmic solution use for allergic rhinitis or allergy associated reddening of the eyes also stabilizes mast cell, has anti-inflam effects only applied topically
34
Cortisol
glucocorticoid, secreted in response to ACTH interact with specific nuclear receptors to increase or decrease the expression of corticoresponsive genes anti-inflammatory effects largely mediated by transrepression --- main mechanism is repression of phospholipase A2; also COX2 & prevents proinflammatory cytokine expression & decreases number of immune cells metabolic effects: upregulation of trangluconeogenesis enzymes inactivated by 11βHSD2 (kidneys) net metabolic effect is increased blood glucose levels Cushings A/E: impairs HPA axis, fluid/electrolyte abnormalities, HTN, hyperglycemia, increased risk for infx, osteoporosis/decreased bone density, myopathy, behavioral disturbances, cataracts, retarded growth, fat redistribution, striae
35
Betamethasone
long acting synthetic corticosteroid; anti-inflammatory effects 25x more potent than cortisol; long half life; no Na+ retention effects; 0.25 equivalent dose to cortisol most commonly used topically for skin infections
36
Dexamethasone
longest acting synthetic corticosteroid; anti-inflammatory effects 25x more potent than cortisol; long half life; no Na+ retention effects; 0.25 equivalent dose to cortisol used for acute adrenal crisis
37
Prednisone
intermediate strength corticosteroid (12-36 hr duration) used for acute organ rejection, chronic adrenal insufficiency, rheumatic diseases, giant cell arteritis, systemic skin diseases (atopic dermatitis), IBD,
38
Triamcinolone
intermediate glucocorticoid used for non-inflammatory joint disease (osteoarthritis), skin diseases (intralesional prep)
39
Metyrapone
cortisol synthesis inhibitor inhibits CYP 11B1 used to treat hypercortisolism, diagnostic tests of HPA axis
40
Ketoconazole
cortisol synthesis inhibitor at high doses, inhibits CYP 17 (to synthesize cortisol & DHEA) ***most effective inhibitor to treat Cushings anti-fungal at low doses
41
Aminoglutethimide
cortisol synthesis inhibitor inhibits CYP 11A (initial & rate-limiting step) used to treat Cushings
42
Aldosterone
endogenous mineralocorticoid synthesized in response to K+ & angiotensin II stimulates renal exchange between Na+/K+ or H+ acts on distal tubules & collecting ducts of kidney to increase reabsorption of Na+ (& thus water) & promote K+ excretion --- results in fluid retention, increased BP increase cardiac fibrosis congenital adrenal hyperplasia commonly caused by CYP 21 mutation --- decreases synthesis of aldosterone
43
Fludrocortisone
mineralocorticoid mineralocorticoid agonist use with corticosteroid in patients with CAH that also have salt wasting
44
Alfentanil
Opioid (class: Phenylpiperadine) DOC for outpatient anesthesia --- repeated doses do not accumulate, recovery is rapid
45
Codeine
opioid (class phenanthrene) prodrug that gets metabolized to morphine by CYP 2D6; chemical modification improves 1st pass survivability potency similar to morphine oral analgesic & anti-tussive
46
Fentanyl
synthetic opioid (phenylpiperadine class) 80-100x greater potency compared to morphine shorter duration highly lipophilic, rapid distribution to other compartments analgesic; improved cardiac stability; not anesthetic fentanyl lollipop used for breakthrough pain
47
Hydrocodone
semi-synthetic opioid (class phenanthrene) greater potency compared to morphine
48
Meperidine
Demerol synthetic opioid (class phenylpiperadine) 1/10 morphine's potency 25% bioavailable used in labor & delivery reduced likelihood of biliary spasm; does not cause miosis toxicity: CNS excitation --- seizure, tremor, convulsions --- metabolite in patients with impaired renal function
49
Methadone
``` synthetic opioid (class phenylheptanone) -one of the highest risk ``` equipotent with morphine high bioavailability once daily dosage, PO longer acting opioid improved risk for heroin addicts some NMDA receptor antagonist properties
50
Morphine
opioid (phenanthrene class) central effects: analgesia, respiratory depression, anti-tussive (suppresses brainstem cough centers) miosis, tolerance, dependence peripheral effects: analgesia, constipation, GI spasm; generally increases smooth muscle tone degranulation of mast cells (which can cause pruritis, systemic hypotension) active metabolites: excitotoxic, analgesic main A/E: respiratory depression; also miosis, coma more effective against continuous, dull pain
51
Oxycodone
semi-synthetic opioid (class phenanthrene) greater potency compared to morphine
52
Remifentanil
synthetic opioid (phenylpiperidine class)
53
Sufentanil
synthetic opioid (phenylpiperidine class)
54
Tapentadol
mixed opioid analgesic moderate mu receptor agonist, NE reuptake inhibitor metabolically stable congener of O-desmethyltramadol
55
Tramadol
mixed opioid analgesic --- 5HT releaser, NE reuptake inhibitor, weak mu opioid receptor agonist O-desmethyltramadol metabolite is a stronger mu agonist (CYP2D6 conversion) toxicity: seziures (NOT respiratory depression)
56
Naloxone
mu opioid antagonist shortest duration of action, not available orally because it gets destroyed in the liver before getting to bloodstream use to treat opioid overdose in healthy subjects does not alter pain threshold but increases hormone secretion hyperalgesic in post surgery patients attenuates/reduces analgesic effects
57
Naltrexone
opioid antagonist longest duration of action available orally addict maintenance
58
Nalmefene
opioid antagonist intermediate duration of action not available orally
59
Diphenhydramine
1st generation antihistamine - prototype inverse agonist of H1 receptor; works best if administered prior to histamine release; also, competitive antagonist for muscarinic receptors crosses BBB very well, causes significant sedation; significant anti-muscarinic effects (dry mouth, tachycardia, blurred vision, constipation) cleared by CYP2D6 most 1st gen antihistamines are metabolized in the liver & excreted in urine in modified form contraindicated in pregnancy
60
Promethazine
1st generation H1 blocker significant central anti-cholinergic --sedative & antiemetic cleared by CYP2D6 commonly used for motion sickness, N/V; rescue agent for migraines A/E skin rash
61
Doxepin
potent H1 antagonist (1st gen) primarily used as anti-depressant drowsiness & anticholinergic effects
62
Fexofenedine
2nd generation H1 blocker (prototype) with longer duration of action active metabolite of terfenidine without QT prolongation minimal sedative & anti-muscarinic activity (similar to loratadine) most 2nd gen antihistamines are excreted in the urine in unmetabolized form
63
Cetirizine
H1 blocker (2nd gen) poor penetration of BBB; sedation is limited; BUT drowsiness is a serious side effect may have benefit in asthma patients useful in pediatric patients
64
Loratadine
2nd generation H1 blocker oral, relatively non-sedating rapidly absorbed by GI tract, converted to active form by CYP450s--- drug interactions does not readily cross BBB; preferentially binds peripheral receptors long duration of action
65
desloratadine
2nd generation H1 blocker active metabolite of loratadine more expensive
66
Olopatadine
new anti-histamine on the horizon nasal spray, ophthalmic solution use for allergic rhinitis or allergy associated reddening of the eyes also stabilizes mast cell, has anti-inflam effects only applied topically
67
Sumatriptan
Prototype Triptan moderate to severe migraine; 1st line therapy; continues to work even once HA has progressed structurally similar to 5HT but different action selective agonist for 5HT1B/D --- inhibits 5HT release reduces release of pro-inflammatory agents in trigeminal nerve; may facilitate anti-nociceptive input to CNS selective AVA pre-capillary vasoconstrictor for meninges --- promote vasoconstriction to reduce headache pain A/E chest pressure/tightness contraindicated in patients with CAD
68
Frovatriptan
triptan with the longest action --- good for prophylaxis of migraine
69
Ergotamine
prototype ergot derivative used in the treatment of migraine; can be used for rescue for intractable migraine often a single formulation with caffeine pressor & hallucinogen through 5HT; D2 receptor agonist --causes N/V abortive anti-migraine; vasoconstrictive effects variably absorbed from GI tract Toxicity: hallucinations, vasospasm, paresthesia, gangrene, abortion
70
Dihydroergotamine
ergot derivative, used in the treatment of migraine; can be used for rescue for intractable migraine poorly, variably absorbed; SL or nasal spray less effective as HA progresses better tolerated than ergotamine (but may have vasospasm, gangrene, hallucinations, abortion)
71
migraine prophylaxis drugs
beta blockers, AEDs, SSRI
72
intractable migraine rescue drugs
ergotamine, dihydroergotamine, opioid, promethazine, metaclopromide
73
Chlorpromazine
typical anti-psychotic; phenothiazine class least potent class greatest sedation effect & weight gain; hypotension the original anti-psychotic
74
Fluphenazine
typical anti-psychotic; phenothiazine class greater potency than chlorpromazine; greater EPS effects, neuroleptic malignant syndrome
75
Thiothixene
typical anti-psychotic; thioxanthene class
76
Haloperidol
typical anti-psychotic; causes greatest EPS, neuroleptic malignant syndrome far more potent among the typicals; causes least amt of weight gain & sedation for typical drugs
77
Clozapine
atypical anti-psychotic alleviates both positive & negative symptoms of schizophrenia; few EPS or sedation less selective for D2 receptors; equal to greater potency at 5HT receptors life-threatenting agranulocytosis, hypotension; last resort drug; more likely to cause weight gain
78
Risperidone
atypical anti-psychotic alleviates both positive & negative symptoms of schizophrenia; few EPS or sedation less selective for D2 receptors; equal to greater potency at 5HT receptors
79
Olanzapine
atypical anti-psychotic causes the greatest weight gain among anti-psychotics alleviates both positive & negative symptoms of schizophrenia; few EPS or sedation less selective for D2 receptors; equal to greater potency at 5HT receptors
80
Quetiapine
atypical anti-psychotic alleviates both positive & negative symptoms of schizophrenia; few EPS or sedation less selective for D2 receptors; equal to greater potency at 5HT receptors
81
Ziprasidone
atypical anti-psychotic does NOT cause weight gain* but does have cardiotoxicity ---arrhythmias alleviates both positive & negative symptoms of schizophrenia; few EPS or sedation less selective for D2 receptors; equal to greater potency at 5HT receptors
82
Aripiprazole
atypical anti-psychotic alleviates both positive & negative symptoms of schizophrenia; few EPS or sedation partial D2 agonist less selective for D2 receptors; equal to greater potency at 5HT receptors
83
adverse effects of anti-psychotics (general)
EPS (tremor, acute dystonia, bradykinesia) akathesia (restlessness, rocking, pacing) tardive dyskinesia: facial & neck tics Neuroleptic malignant syndrome: fever, rigidity, cognitive changes ---treat with muscle relaxant cardiac arrhythmias weight gain hypotension anti-muscarinic effects (dry mouth, constipation, difficulty urinating, loss of accommodation) amenhorrhea/galactorrhea syndrome & infertility sedation confusion, attention/learning deficits blunt affect, lack of pleasure, dysphora anti-emetic **mainly associated with reduced DA activity
84
CNS stimulant effects
increased sympathetic output increased alertness, wakefulness, attention appetite suppression euphoria, exhilaration, self-confidence
85
Nicotine
CNS stimulant -alkaloid derived from plants, esp tobacco reaches brain within seconds when smoked stimulates epinephrine release from adrenal gland stimulates glutamateric neurons in laterodorsal tegmental area to release glutamate onto VTA neurons, which causes them to release DA in the nucleus accumbens --nicotine mimics ACh at nACh receptors can cause sudden infant death syndrome if used in pregnancy treatment for addition: nicotine replacement, bupropion, varenicline withdrawal symptoms: agitation, anger, frustration
86
Bupropion
noncompetitive nicotine receptor antagonist & dopamine reuptake blocker commonly used as an anti-depressant
87
Varenicline
partial nicotine receptor agonist
88
Cocaine
CNS stimulant blocks reuptake of DA by blocking DAT increased sympathetic output, hyperthermia, increased vasoconstriction acute psychosis cardiotoxicity --- increased HR & contractility, constriction of coronary arteries; can also block Na+ channels causing arrhythmias (due to anesthetic effect) with prolonged use, develop syndrome similar to parkinson's -- depletion of DA
89
Amphetamines
CNS stimulant overall: promotes DA/NE in the synapse specific: blocks monoamine transport into vesicles blocks reuptake of monoamines (DA, NE) blocks monoamine oxidase blocks DAT (internalization of the transporter) promotes vesicle release into synapse increased sympathetic output, hyperthermia, increased vasoconstriction, acute psychosis, cardiotoxicity (increased HR & contractility) tachyphylaxis -- due to depletion of DA & NE
90
MDMA, Ecstasy
CNS stimulant re-uptake blocker of monoamines, preferentially 5HT inhibits transport of monoamines into presynaptic vesicles, causing reverse transport into synapse effects: amphetamine/psychedelic effects--- euphoria, increased psychomotor output, increased sympathetic acitivity, mild perceptual disturbances, hallucinations, increased connectiviity with surroundings A/E meth mouth rapid tolerance serotonin syndrome: ecstasy causes large release of 5HT into synapse & blocks its reuptake --- hyperthermia, sweating, nausea, tachycardia, HTN; muscle spasms twitches; confusion, mania, hallucinations, agitation, coma, HA; dehyrdation
91
Bath Salts (MDPV)
CNS stimulant, synthetic based on cathinone, from the khat shrub similar action to amphetamines; also block 5HT uptake & may activate 5HT2A receptors effects: euphoria, increased CNS output, appetite suppression; perceptual disturbances, hallucinations toxicity similar to other CNS stimulants but causes more severe agitation & paranoia, self-destructive, violent behavior, psychosis
92
Alcohol
binds to & GABA receptors & enhances GABA effect (in the presence of GABA); inhibits NMDA retards development & learning & memory positive & negative reinforcement -alcohol increases firing rate of VTA dopaminergic neurons (by disinhibition) metabolic tolerance withdrawal can be serious; 1st phase; 2nd phase: hyperthermia -- causing big increase in BP & tachycardia hepatotoxicity, cardiac dysfunction wernicke korsakoff: caused by thiamin deficiency --ataxia, paralysis of eye muscles, confusion, may lead to coma; later; memory impairment
93
Disulfiram
inhibits alcohol dehydrogenase; causes acetaldehyde to build up, which causes nausea when consuming alcohol
94
Acamprosate
blocks NMDA receptors & activates GABA used to treat alcoholism
95
Topiramate
blocks AMPA/kainate receptors & activates GABA used to treat alcoholism
96
Fluoxetine
SSRI; used for alcoholism & depression
97
Fomepizole
inhibits alcohol dehydrogenase; for methanol ethylene glycol poisoning
98
Benzodiazepine, oxazepam
sedative; often prescribed with methadone to counteract sympathetic rebound in treating opioid withdrawal; cause sedation, respiratory depression
99
Buprenoprhine
partial mu receptor agonist (causes euphoria); & a kappa receptor antagonist (prevents dysphoria) produces euphoric effects when taken on its own so you're less likely to experience withdrawal effects from opioids if crushed & injected IV, nalaxone blocks its effects, preventing it from getting into the brain if taken SL as it should be, naloxone is inactivated & it can have full central effects (it can get into the brain)
100
LSD
psychedelic hallucinogen 5HT1A/2 partial agonist inihibits GABA release & causes disinhibition of DA release dizziness, nausea, numbness, increased sympathetic output, ataxia; intense feelings of euphoria, insight, deep connection to environment; hallucinations
101
psilocin & psylocybin
psychedelic hallucinogen, found in mushrooms 5HT1A/2 partial agonist inihibits GABA release & causes disinhibition of DA release dizziness, nausea, numbness, increased sympathetic output, ataxia; intense feelings of euphoria, insight, deep connection to environment; hallucinations
102
PCP (Phencyclidine)
synthetic dissociative hallucinogen; derived from ketamine open NMDA glutamate receptor blocker in the brain delirium (vivid hallucinations, dissociation of mind from body; agitation, aggression; very difficult to deal with) psychotic behavior **Olney's lesions: NMDA receptor antagonist neurotoxicity = vacuolization of cortical neurons, gliosis, dementia; also neuronal apoptosis
103
THC
marijuana reduces intraocular pressure, stimulates appetite binds & activates cannabinoid receptors (similar to opioids) mild hallucinations, euphoria, ataxia, impaired judgment, memory impairment, reduced attention; mellowness, tranquil toxicity/OD risk is low bad trips--> flashback = hallucinogen persisting perception syndrome slacker syndrome can potentiate the effects of CNS depression used as an anti-emetic in cancer chemo (Dronabinol)
104
inhalants (NO, household solvents)
produce CNS depression; brief head rush due to rapid vasodilation, euphoria, dizziness, motor disturbances; HA, fainting, nausea toxicity: asphyxiation; respiratory depression, hepato, nephro, neuro toxicity; pulmonary disease, bone marrow suppression
105
L DOPA
dopamine precursor; 1st line drug for PD can cross the BBB, & gets converted to DA by DOPA decarboxylase efficacy decreases with time almost never given alone because the gut also contains DOPA decarboxylase peripheral side effects due to conversion to DA - GI disturbances; give anti-emetic - tachycardia, hypotension - reduced delivery to CNS central effects: "wearing off", "on/off" abnormal involuntary movements psychomimetic vitamin B6 enhances metabolism can have HTN crisis if used in combination with MAOI
106
Carbidopa
dopa decarboxylase inhibitor; used to treat PD, often given in combination with L-DOPA does NOT cross BBB; but improves L-DOPA delivery to CNS; reduces DA-mediated peripheral side effects (nausea, CV)
107
Sinemet
= L-DOPA + Carbidopa increased delivery of L-DOPA to CNS with fewer peripheral side effects
108
Entacapone
COMT inhibitor; used in combination with L-DOPA & Carbidopa to treat PD lower toxicity, does NOT cross BBB COMT is enzyme that produces 3OMD that competes with L-DOPA for transport into CNS
109
Stalevo
L-DOPA + Carbidopa + Entacapone
110
Bromocriptine
DA agonist, ergo based used in treatment of PD selective D2 agonist; excreted in bile & feces can be used as an anti-psychotic to help restore the DA imbalance, especially in neuroleptic malignant syndrome
111
Pramipexole
non-ergot based DA agonist greatest affinity for D3 receptor but partial agonist (also D2, D4) antioxidant free radical scavenger -- neuroprotection excreted by the kidney dosed 3x/day, requires slow titration effective monotherapy for PD; effective adjunct that helps relieve on/off phenomenon in moderate to severe PD
112
Ropinerole
non-ergot based DA greatest affinity for D2 receptor (but also D3, D4) metabolized by CYP1A2 dosed 3x/day, requires slow titration effective monotherapy for PD; effective adjunct that helps relieve on/off phenomenon in moderate to severe PD
113
Apomorphine
PD rescue drug potent, non-selective DA agonist induces vomiting, temporary relief of off state delivered SQ, rapidly distributes to CNS A/E nausea; very poorly tolerated
114
Selegilline
monoamine oxidase B inhibitor --- inhibits metabolism of DA; used to treat PD mood elevation, nausea, dry mouth, confusion, adverse reactions with meperidine, TCAs & SSRIs blocks MPTP toxicity may cause early death
115
Amantidine
MAO inhibitor used as adjunct with Sinemet; treat PD short lived effect but can improve dyskinesias in severe PD A/E livedo retiularis, peripheral edema
116
Benztropine Mesylate
Muscarinic receptor antagonist; used to treat PD --- reducing ACh input to striatal muscarinic receptors helps balance ACh/DA some reduction of tremor & rigidity A/E excitement, confusion, hallucination, anti-cholinergic effects (tachycardia, xerostomia, etc)
117
Tacrine
inhibits AChE & butrylcholinesterase metabolized by CYP1A2 zero order kinetics -- 1st pass enzyme saturation hepatotoxicity, N/V/D, agitation, rash, anorexia, confusion overdose: cholinergic stimulation (lacrimation, vomiting, diarrhea, salivation, tremor, etc)--- antidote: atropine
118
Donezepil
AChE inhibitor completely bioavailable long half life highly protein bound better tolerated than tacrine
119
Galantamine
nicotinic receptor stimulator; used to treat AD
120
Memantine
NMDA receptor antagonist; used to treat AD
121
Corticosterone
corticosteroid, immunosuppressant primary action: reduce peripheral immune cells (& inflammation)
122
Prednisolone
the active metabolite of prednisone often used for pulse therapy at high doses in treating acute rejection oral systemic for asthma exacerbations
123
Pimecromulus
calcineurin inhibitor -- blocks immunophilins --- thereby prevents activation of NFAT less readily absorbed (so fewer systemic effects) & don't prevent certain immune cell interactions compared to corticosteroids good at preventing acute transplant rejection nephrotoxicity, HTN, diabetes, neurotoxicity, lymphoproliferative disease, GI problems preferred CI for children; & for mild to moderate atopic dermatitis metabolized by CYP3A system, eliminated mainly in bile/feces
124
cyclosporin
calcineurin inhibitor --- thereby prevents activation of NFAT less readily absorbed (so fewer systemic effects) & don't prevent certain immune cell interactions compared to corticosteroids good at preventing acute transplant rejection metabolized by CYP3A system, eliminated mainly in bile/feces nephrotoxicity, HTN, diabetes, neurotoxicity, lymphoproliferative disease, GI problems A/E specific to cyclosporin: hirsutism, gingival hyperplasia
125
Tacrolimus
calcineurin inhibitor --- binding to immunophilins -- thereby prevents activation of NFAT most potent; good at preventing acute transplant rejection metabolized by CYP3A system, eliminated mainly in bile/feces nephrotoxicity, HTN, diabetes, neurotoxicity, lymphoproliferative disease, GI problems A/E specific to tacrolimus: myocyte hypertrophy, diabetes
126
Azathioprine
cytotoxic immunosuppressant -- inhibits de novo synthesis of purines --- inhibits enzyme responsible for PRPP-->IMP - also prevents salvage pathway purine synthesis - -- forms TIMP, which makes DNA labile and break down active metabolite: 6MP -broken down by TPMT & XO allopurinol inhibits XO --> increases 6 MP may have carcinogenic effects, teratogenicity all cytotoxic drug A/E: leukopenia, thrombocytopenia, N/V, hepatotoxicity
127
Mycophenylate mofetil
cytotoxic immunosuppressant -- inhibits de novo synthesis of purines -- prevents IMP-->GMP quickly metabolized to MPA (GI) -->MPAG (liver) by glucuronyltransferase MPA competes with MPAG --- causes increased clearance of free MPA 2 peak concentration levels due to enterohepatic recycling preferred drug for induction phase fewer toxic profile/adverse effects mainly A/E is diarrhea very highly bioavailable all cytotoxic drug A/E: leukopenia, thrombocytopenia, N/V, hepatotoxicity
128
Sirolimus
cytotoxic immunosuppressant --- causes cell cycle arrest (in G1) by binding to MTORs longer elim half life; extensively metabolized into 7 inactive molecules A/E hypercholesterolemia, impaired wound healing metabolized by CYP450s; similar drug interactions to the calcineurin inhibitors all cytotoxic drug A/E: leukopenia, thrombocytopenia, N/V, hepatotoxicity
129
Rho immune globulin
Ab against Rh (D) Ag on RBCs used in erythroblastosis fetalis -- give to Rh negative mothers to prevent immune system attack on subsequent fetuses
130
antithymocyte globulin (thymoglobulin)
polyclonal Ab prepared from animals binds to T cell surface proteins & rapidly leads to depletion of T & B cells A/E leukopenia, thrombocytopenia cytokine release sydrome: N/V/D, fever & chills, myalgias/arthralgias, anaphylaxis most commonly used Ab in therapy
131
Muronumab
binds to CD3 & rapidly leads to depletion of CD3+ cells (mainly T cells) A/E cytokine release syndrome: binding of drug causes T cells to become activated & release cytokines -N/V/D, fever/chills/arthralgias/myalgias, anaphylaxis? also CNS effects: sz, encephalopathy, cerebral edema,
132
Daclizumab
IL-2 Ab binds to alpha subunit of IL-2 receptor & antagonizes IL-2 binding --- prevents proliferation & differentiation of T & B cells longer half life & saturates receptor for a longer time (compared to basilixumab) A/E hypersensitivity reactions used for prophylaxis for allograft rejection; used in almost all new lung transplant patients for induction therapy rarely for maintenance therapy
133
Basilixumab
IL-2 Ab binds to alpha subunit of IL-2 receptor & antagonizes IL-2 binding --- prevents proliferation & differentiation of T & B cells A/E hypersensitivity reactions used for prophylaxis for allograft rejection; used in almost all new lung transplant patients for induction therapy rarely for maintenance therapy
134
Infliximab
anti-TNFa --- causes profound anti-inflammatory effects used for Crohn's, ulcerative colitis, psoriatic & rheum arthritis A/E hypersensitivity reactions
135
Etanercept
anti-TNFa used for severe psoriasis & psoriatic & rheum arthritis fusion protein between human TNFa & human IgG
136
Albuterol
inhaled, short acting β2 agonist -- DOC for acute asthma attack
137
Salbutamol
inhaled or oral, short acting β2 agonist -- DOC for acute asthma attack oral A/E: skeletal muscle tremor, nervousness, restlessness, anxiety, tachycardia, arrhythmias, angina, N/V
138
Levalbuterol
inhaled, short acting β2 agonist -- DOC for acute asthma attack a newer drug; R isomer of albuterol fewer adverse effects but more expensive
139
Terbutaline
inhaled or oral, short acting β2 agonist use for treatment of acute asthma attack oral A/E: skeletal muscle tremor, nervousness, restlessness, anxiety, tachycardia, arrhythmias, angina, N/V
140
Salmeterol
inhaled, long acting β2 agonist long side chain inserts into PM & gradually diffuses 50x more selective to β2 receptors than albuterol not used in monotherapy; used with corticosteroids
141
Formoterol
inhaled, long acting β2 agonist long side chain inserts into PM & gradually diffuses not used in monotherapy; used with corticosteroids
142
Beclomethasone
inhaled corticosteroid; used in treatment of asthma
143
Budesonide
inhaled corticosteroid; used in treatment of asthma
144
Flunisolide
inhaled corticosteroid; used in treatment of asthma
145
Fluticasone
inhaled corticosteroid; used in treatment of asthma
146
Mometasone
inhaled corticosteroid; used in treatment of asthma
147
ipratropium bromide
anti-cholinergic agent -- competitive inhibitor of M3 ACh receptors --- block contraction to airway smooth muscle (vasodilation) derivative of atropine can be combined with beta 2 agonist (albuterol) minimal A/E: dry mouth, blurred vision, urinary retention, bitter taste, glaucoma
148
tiotropium bromide
anti-cholinergic agent -- competitive inhibitor of M3 ACh receptors --- block contraction to airway smooth muscle (vasodilation) new; dry powder inhaler, longer duration can be combined with beta 2 agonist (albuterol) minimal A/E: dry mouth, blurred vision, urinary retention, bitter taste, glaucoma
149
Hydrocortisone
as topical cream is low potency; used for mild skin infections IV form is for oral systemic asthma exacerbations & enemas fluid retention, weight gain (increased appetite), osteoporosis, skin bruising, hypertension, cataracts, diabetes, peptic ulcers, psychosis, susceptibility to infections, HPA suppression (adrenal, GH) --taper off
150
cromolyn sodium
mast cell degranulation inhibitor anti-inflammatory: inhibits cough by inhibiting airway nerves, inhibits degranulation of mast cells, inhibits eosinophils use prophylactically for asthma, less effective than corticosteroids reduces hyperreactivity Poorly absorbed A/E: laryngeal edema, joint swelling, headache, rash, nausea
151
nedocromil sodium
mast cell degranulation inhibitor anti-inflammatory: inhibits cough by inhibiting airway nerves, inhibits degranulation of mast cells, inhibits eosinophils reduces hyperreactivity Poorly absorbed use prophylactically for asthma, less effective than corticosteroids A/E: laryngeal edema, joint swelling, headache, rash, nausea
152
Omalizumab
anti-IgE, anti-inflammatory binds free IgE, preventing allergic reaction (such as secretion of cyt LTs, which are potent bronchoconstrictors) single SQ injection every 2-4 wks but is very expensive well tolerated A/E rare -- anaphylaxis, malignancy
153
zafirlukast
leukotriene receptor antagonist -- competitive inhibitor of cys-LT1 receptor --- blocks leukotriene action on smooth muscle, mast cells, eosinophils inhibits bronchoconstriction & inflammatory response 2nd line therapy for moderate to severe asthma prophylactic, not rescue or reliever interacts with warfarin, causing increased clotting times A/E HA, N/V, Gi upset, skin rash, abnormal liver function *Churg Strauss Syndrome: eosinophilia in lungs, vasculitis, flu-like sx
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montelukast
leukotriene receptor antagonist -- competitive inhibitor of cys-LT1 receptor --- blocks leukotriene action on smooth muscle, mast cells, eosinophils allows for once daily dosing rather than twice longer acting fewer side effects than zafirlukast A/E HA, N/V, Gi upset, skin rash, abnormal liver function *Churg Strauss Syndrome: eosinophilia in lungs, vasculitis, flu-like sx
155
zileuton
leukotriene synthesis inhibitor --- 5'lipoxygenase inhibitor inhibits synthesis of all leukotrienes A-E4; C, D, E = bronchoconstrictors B = chemoattractant for WBCs inhibits bronchoconstriction & WBC chemoattraction A/E HA, N/V, Gi upset, skin rash, abnormal liver function *Churg Strauss Syndrome: eosinophilia in lungs, vasculitis, flu-like sx also: acute liver disease, decreases clearance of theophylline & warfarin
156
Theophylline
adenosine receptor blocker activates HDACs PGE inhibitor CNS stimulant, CV stimulant, bronchodilator crosses placenta, gets into breast milk eliminated by the liver A/E arrhythmias --- fatal intoxication if taken too fast -HA, palpitation, nausea, dizziness, hypotension, tachycardia, agitation, emesis, restlessness, sz, behavioral toxicity
157
Aspirin
irreversible inhibitor of COX low dose cardioprotector (anti-platelet) moderate dose: analgesic & anti-pyretic high dose: anti-inflammatory A/E: HA/tinnitus, hyperthermia, hyperventilation, salt & water retention; hepatotoxicity *stimulates respiratory center increases temperature by CV effects rather than hypothalamus
158
Indomethacin
NSAID, COX1 > COX2 ; used for closure of patent ductus arteriosus
159
Ibuprofen
NSAID, COX1~COX2 most common topical dental pain
160
Naproxen
NSAID, COX1~COX2 long half life can be alternative anti-platelet drug
161
Diflunisal
NSAID, COX1~COX2 effective for bone cancer & dental surgery; does NOT cross BBB
162
Diclofenac
NSAID, COX 2> COX1 goes into synovial fluid
163
Celecoxib
NSAID, COX 2> COX1 anti-inflammatory without GI effects sulfa drug --- SJS, TEN do NOT use in patients with CV problems
164
Acetominophen
analgesic & antipyretic weak COX inibitor good for osteoarthritis, patients who shouldnt take ASA toxicity: hepatotoxicity due to toxic metabolite
165
N-acetylcysteine
antidote for acetominophen overdose provides SH groups to detoxify the metabolite & restore glutathione levels
166
Omeprazole
proton pump inhibitor enteric coated absorbed from small intestine into bloodstream; secreted into acidic canaliculi, gets protonated then converted to OM-sulfenamide which covalently binds to H+/K+ ATPase short plasma half life but therapeutic effects last for life of pump metabolized by CYP2C19 also inhibits CYP2C19, which slows their metabolism; this also prevents activation of clopidogrel, which prevents clotting (so you increase clotting risk) A/E increased risk for infection due to increased pH, decreased absorption of B12; risk for rebound hypersecretion permits healing
167
Cimetidine
Reversible, competitive H2 antagonist --prevents production of acid by parietal cells not as effective as PPI but allows for quicker response hepatic & renal excretion A/E confusion, depression, hallucination *inhibits some CYPs; anti-androgenic, fast IV bradycardia can use prior to surgery to prevent chemical pneumonitis risk for rebound hypersecretion; increased pH
168
Ranitidine
Reversible, competitive H2 antagonist --prevents production of acid by parietal cells not as effective as PPI but allows for quicker response allowed for BID rather than QID hepatic & renal excretion A/E confusion, depression, hallucination can use prior to surgery to prevent chemical pneumonitis risk for rebound hypersecretion; increased pH
169
Anatacids
ions bind acid and form salt + water aluminum causes constipation, magnesium causes diarrhea cause flatulence due to release of CO2 safe in pregnancy
170
Bismuth Subsalicylate
cytoprotective agent coats erosion, may stimulate PGE A/E black stool & oral cavity
171
Sucralfate
cytoprotective agent --- aluminum hydroxide complex of sulfated sucrose forms viscous paste-like layer in acidic environment --- efficacy is reduced by H2 blockers, PPI, antacids stimulates PGE A/E constipation does NOT raise pH --- can use with patients at higher risk of infection; oral mucositis safe in pregnancy
172
Misoprostol
PGE Agonist inhibits acid secretion & increases mucus, bicarb, blood flow, promotes healing A/E diarrhea, abd pain, abortifacient **prevents PUD in chronic NSAID user
173
Sulfasalazine
5-ASA-like drug -prodrug converted to mesalamine (5-ASA) used to treat IBD -- esp UC inhibits formation of inflammatory mediators such as NFkB & lipoxygenase pathways A/E allergic rxn (possibly SJS) -- sulfapyridine metabolite; also bone marrow suppression safe in pregnancy
174
Mesalamine
5-ASA; activated early in intestine; controlled release; used to treat IBD
175
Balsalazide
5-ASA-like drug; bacterial cleavage in colon
176
Olsalazine
5-ASA-like drug; bacterial cleavage in colon
177
Scopolamine
Muscarinic antagonist -- anti-emetic drug A/E visual disturbances, sedation
178
Dimenhydrinate
Dramamine -- H1 antagonist used for anti-emetic purposes A/E visual disturbances, sedation
179
Ondansetron
anti-emetic for cancer chemo; 5HT3 antagonist A/E diarrhea, HA
180
Aprepitant
anti-emetic for cancer chemo; blocks neurokinin receptor for substance P A/E fatigue, dizziness, diarrhea
181
Metoclopromide
anti-emetic for cancer chemo; D2/5HT3 Antagonist, M agonist --- anti-emetic & prokinetic A/E fatigue, insomnia, Parkinson-like sx, acute dystonia, extrapyramidal reaction
182
Dronabinol
anti-emetic cannabinoid; used for cancer chemo A/E drowsiness, ataxia, hyperphagia, disoriented, anxiety, psychosis
183
Psyllium
laxative -- bulk & stool softener effect in 1-3 days
184
Senna
laxative -- cathartic; stimulant & low dose osmotic; effect in 6-8 hrs
185
polyethylene glycol electrolyte solution
purgative laxative -- water evacuation; non-absorbable, isotonic, osmotic
186
Loperamide
anti-diarrheal opioid does NOT cross BBB; used for IBS + diarrhea
187
Dicyclomine
anti-muscarinic anti-diarrheal decreased peristalsis, antispasmodic
188
probiotics
recolonize intestine with bacteria
189
Lubipristone
PGE derivative -- activates Cl- channels in GI tract, increasing intestinal fluid secretion