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54 Cards in this Set

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Levodopa (Dopar) - Indication
Used for treatment in PD (Parkinson’s disease)
Levodopa (Dopar) - Action
is converted to dopamine in the CNS, where it serves as a neurotransmitter. Carbidopa, a decarboxylase inhibitor, prevents peripheral destruction of levodopa.
Levodopa (Dopar)- Pharmacokinetics
administered orally and undergoes rapid absorption from the small intestine.

Widely distributed. Levodopa--enters the CNS in small concentrations. Carbidopa--does not cross the blood-brain barrier

Levodopa--mostly metabolized by the GI tract and liver. Carbidopa --30% excreted unchanged by the kidneys.

Half-life: Levodopa--1 hr; carbidopa--1-2 hr.
Levodopa (Dopar)- Adverse effects
e. CNS: involuntary movements, anxiety, dizziness, hallucinations, memory loss, psychiatric problems.
EENT: blurred vision, mydriasis.
GI: nausea, vomiting, anorexia, dry mouth, hepatotoxicity.
Derm: melanoma.
Hemat: hemolytic anemia, leukopenia. Misc: darkening of urine or sweat.
Levodopa (Dopar)- onset, peak, duration
Levodopa 10-15 min unknown 5-24 hr or more
Carbidopa/levodopa sustained release unknown 2 hr 12 hr
Levodopa (Dopar)- route/dosage
PO (Adults): 250 mg 2-4 times daily; may increase by 100-750 mg q 3-7 days until desired effect is achieved (not to exceed 8 g/day).
Zolpidem (Ambien) - Indications
Insomnia
Zolpidem (Ambien) - Action
Produces CNS depression by binding to GABA receptors. Has no analgesic properties.
Zolpidem (Ambien) - Pharmacokinetics
Rapidly absorbed following oral administration
distribution not known
Converted to inactive metabolites, which are excreted by the kidneys.
Half-life: 2.5-2.6 hr (increased in geriatric patients and patients with hepatic impairment)
Zolpidem (Ambien) - onset, peak, duration
PO rapid 30 min-2 hr 6-8 hr
PO-ER rapid 2-4 hr 6-8 hr
Zolpidem (Ambien) - Adverse effects
b. CNS: abnormal thinking, amnesia, behavior changes, daytime drowsiness, dizziness, "drugged" feeling, hallucinations, sleep-driving.
GI: diarrhea, nausea, vomiting.
Misc: ANAPHYLACTIC REACTIONS, hypersensitivity reactions, physical dependence, psychological dependence, tolerance.
Zolpidem (Ambien) - Route/dosage
PO (Adults): Tablets-10 mg at bedtime; extended-release tablets -- 12.5 mg at bedtime.
Geri - cut in half
Morphine Sulfate - Indication
Severe pain.
Pulmonary edema.
Pain associated with MI.
Morphine Sulfate - Action
Binds to opiate receptors in the CNS. Alters the perception of and response to painful stimuli while producing generalized CNS depression.
Morphine Sulfate - Pharmacokinetics
Variably absorbed (about 30%) following oral administration. More reliably absorbed from rectal, subcut, and IM sites.
Widely distributed. Crosses the placenta
Protein Binding
Mostly metabolized by the liver. Active metabolites excreted renally.
Half-life: Adults 2-4 hr
Morphine Sulfate - Adverse effects
d. CNS: confusion, sedation, dizziness, dysphoria, euphoria, floating feeling, hallucinations, headache, unusual dreams.
EENT: blurred vision, diplopia, miosis.
Resp: RESPIRATORY DEPRESSION.
CV: hypotension, bradycardia.
GI: constipation, nausea, vomiting.
GU: urinary retention.
Derm: flushing, itching, sweating.
Misc: physical dependence, psychological dependence, tolerance.
Morphine Sulfate - peak, onset, duration
PO unknown 60 min 4-5 hr
PO-ER, SR unknown 3-4 hr 8-24 hr
IM 10-30 min 30-60 min 4-5 hr
Subcut 20 min 50-90 min 4-5 hr
Rect unknown 20-60 min 3-7 hr
IV rapid 20 min 4-5 hr
Epidural 6-30 min 1 hr up to 24 hr (48 hr for liposomal injection)
IT rapid (min) unknown up to 24 hr
Morphine Sulfate - Route/dosage
PO, Rect - 30 mg q 3-4 hr initially or once 24-hr opioid requirement is determined
IM IV, Subcut - for moderate to severe pain in opioid-naive patients--4-10 mg q 3-4 hr. MI--8-15 mg, for very severe pain additional smaller doses may be given every 3-4 hr.
Continuous infusion--0.8-10 mg/hr; may be preceded by a bolus of 15 mg
Epidural (Adults): Intermittent injection--5 mg/day (initially); if relief is not obtained at 60 min, 1-2 mg increments may be made; (total dose not to exceed 10 mg/day. Continuous infusion--2-4 mg/24 hr
Prozac (sarafem) - indication
Various forms of depression.
OCD.
Bulimia nervosa.
Panic disorder.
Sarafem: Management of premenstrual dysphoric disorder (PMDD).
Prozac (sarafem) - Action
Selectively inhibits the reuptake of serotonin in the CNS.
Prozac (sarafem) - Pharmacokinetics
Well absorbed after oral administration
Crosses the blood-brain barrier.
Protein Binding: 94.5%.
converted by the liver to norfluoxetine, another antidepressant compound
12% excreted by kidneys as unchanged fluoxetine, 7% as unchanged norfluoxetine.
Half-life: 1-3 days (norfluoxetine 5-7 days).
Prozac (sarafem) - onset, peak, duration
PO 1-4 wk unknown 2 wk
Prozac (sarafem) - adverse reactions
d. CNS: SEIZURES, anxiety, drowsiness, headache, insomnia, nervousness, abnormal dreams, dizziness, fatigue, hypomania, mania, weakness.
EENT: stuffy nose, visual disturbances.
Resp: cough.
CV: chest pain, palpitations.
GI: diarrhea, abdominal pain, abnormal taste, anorexia, constipation, dry mouth, dyspepsia, nausea, vomiting, weight loss.
GU: sexual dysfunction, urinary frequency.
Derm: excessive sweating, pruritus, erythema nodusum, flushing, rashes.
Endo: dysmenorrhea. MS: arthralgia, back pain, myalgia.
Neuro: tremor.
Misc: allergic reactions, fever, flu-like syndrome, hot flashes, sensitivity reaction.
Prozac (sarafem) - Route/dosage
20 mg/day in the morning. After several weeks, may increase by 20 mg/day at weekly intervals. Doses greater than 20 mg/day should be given in 2 divided doses, in the morning and at noon (not to exceed 80 mg/day)
Alprazolam (Xanax) - Indication
Treatment of Generalized Anxiety Disorder (GAD).
Panic Disorder.
Management of anxiety associated with depression.
Alprazolam (Xanax) - Action
Acts at many levels in the CNS to produce anxiolytic effect.
May produce CNS depression.
Effects may be mediated by GABA, an inhibitory neurotransmitter.


(benzodiazepines)
Alprazolam (Xanax) - Pharmacokinetics
Well absorbed (90%) from the GI tract;
Widely distributed, crosses blood-brain barrier.
Metabolized by the liver (CYP3A4 enzyme system)
Half-life: 12-15 hr.
Alprazolam (Xanax) - onset, peak, duration
PO 1-2 hr 1-2 hr up to 24 hr
Alprazolam (Xanax) - Adverse effects
d. CNS: dizziness, drowsiness, lethargy, confusion, hangover, headache, mental depression, paradoxical excitation.
EENT: blurred vision.
GI: constipation, diarrhea, nausea, vomiting, weight gain.
Derm: rashes.
Misc: physical dependence, psychological dependence, tolerance.
Alprazolam (Xanax) - Route/dosage
Anxiety
PO (Adults): 0.25-0.5 mg 2-3 times daily (not >4 mg/day
Panic Attacks
PO (Adults): 0.5 mg 3 times daily; may be increased by 1 mg or less every 3-4 days as needed (not >10 mg/day).
Triptan (Imetrex) - Indications
Acute treatment of migraine attacks.
Subcut: Acute treatment of cluster headache episodes.
Triptan (Imetrex) - Action
Acts as a selective agonist of 5-HT1 at specific vascular serotonin receptor sites, causing vasoconstriction in large intracranial arteries.
Triptan (Imetrex) - Pharmacokinetics
Well absorbed (97%) after subcut administration. Absorption after oral administration is incomplete and significant amounts undergo substantial hepatic metabolism, resulting in poor bioavailability (14%). Well absorbed after intranasal administration.

Does not cross the blood-brain barrier

Mostly metabolized (80%) by the liver.

Half-life: 2 hr.
Triptan (Imetrex) - onset, peak, duration
PO within 30 min 2-4 hr up to 24 hr
Subcut 30 min up to 2 hr up to 24 hr
Nasal within 60 min 2 hr unknown
Triptan (Imetrex) - adverese effects
d. CNS: dizziness, vertigo, anxiety, drowsiness, fatigue, feeling of heaviness, feeling of tightness, headache, malaise, strange feeling, tight feeling in head, weakness.
EENT: alterations in vision, nasal sinus discomfort, throat discomfort.
CV: MI, angina, chest pressure, chest tightness, coronary vasospasm, ECG changes, transient hypertension.
GI: abdominal discomfort, dysphagia.
Derm: tingling, warm sensation, burning sensation, cool sensation, flushing.
Local: injection site reaction. MS: jaw discomfort, muscle cramps, myalgia, neck pain, neck stiffness.
Neuro: numbness.
Triptan (Imetrex) - route/dosage
PO (Adults): 25 mg initially; if response is inadequate at 2 hr, up to 100 mg may be given If headache recurs, doses may be repeated q 2 hr (not to exceed 300 mg/day).

Subcut (Adults): 6 mg; may repeat after 1 hr (not to exceed 12 mg in 24 hr).

Intranasal (Adults): Single dose of 5, 10, or 20 mg in one nostril; may be repeated in 2 hr, not to exceed 40 mg/24 hr or treatment of >5 episodes/mo
Valproic Acid (Depakote) - Indication
Monotherapy and adjunctive therapy for simple and complex absence seizures.
Monotherapy and adjunctive therapy for complex partial seizures.
Adjunctive therapy for patients with multiple seizure types, including absence seizures.
Divalproex sodium only: Manic episodes associated with bipolar disorder, Prevention of migraine headache .
Valproic Acid (Depakote) - Action
Increase levels of GABA, an inhibitory neurotransmitter in the CNS.
Valproic Acid (Depakote) - Pharmacokinetics
Well absorbed following oral administration; . IV administration results in complete bioavailability.

Rapidly distributed into plasma and extracellular water. Cross blood-brain barrier

Protein Binding: 80-90%,

Mostly metabolized by the liver; minimal amounts excreted unchanged in urine.

Half-life: Adults: 9-16 hr.
Valproic Acid (Depakote) - onset, peak, duration
PO--liquid 2-4 days 15-120 min 6-24 hr
PO--capsules 2-4 days 1-4 hr 6-24 hr
PO--delayed-release products 2-4 days 3-5 hr 12-24 hr
PO--extended-release products 2-4 days 7-14 hr 24 hr
IV 2-4 days end of infusion 6-24 hr
Valproic Acid (Depakote) - adverse effects
d. CNS: agitation, dizziness, headache, insomnia, sedation, confusion, depression.
CV: peripheral edema.
EENT: visual disturbances.
GI: HEPATOTOXICITY, PANCREATITIS, abdominal pain, anorexia, anorexia, diarrhea, indigestion, nausea, vomiting, constipation, increased appetite.
Derm: alopecia, rashes.
Endo: weight gain. Hemat: leukopenia, thrombocytopenia. Metab: HYPERAMMONEMIA.
Neuro: tremor, ataxia.
Valproic Acid (Depakote) - route/dosage
po - Initial dose of 10-15 mg/kg/day in 1-4 divided doses; ↑ by 5-10 mg/kg/day weekly until therapeutic response achieved (not to exceed 60 mg/kg/day);

IV (Adults and Children): Give same daily dose and at same frequency as was given orally; switch to oral formulation as soon as possible.

Rect (Adults and Children): Dilute syrup 1:1 with water for use as a retention enema. Give 17-20 mg/kg load, maintenance 10-15 mg/kg/dose q 8 hr. Mood Stabilizer


Depakote--Initial dose of 750 mg/day in divided doses initially, titrated rapidly to desired clinical effect or trough plasma levels of 50-125 mcg/ml (not to exceed 60 mg/kg/day)
Naloxone (Narcan) - Indication
Reversal of CNS depression and respiratory depression because of suspected opioid overdose
Naloxone (Narcan) - Action
Competitively blocks the effects of opioids, including CNS and respiratory depression, without producing any agonist (opioid-like) effects.
Naloxone (Narcan) - Phramacokinetics
Well absorbed after IM or subcut administration

Rapidly distributed to tissues.

Metabolized by the liver.

Half-life: 60-90 min
Naloxone (Narcan) - onset, peak, duration
IV 1-2 min unknown 45 min
IM, Subcut 2-5 min unknown >45 min
Naloxone (Narcan) - adverse effects
d. CV: hypertension, hypotension, ventricular fibrillation, ventricular tachycardia.
GI: nausea, vomiting.
Naloxone (Narcan) - route/dosage
IV (Adults): 0.02-0.2 mg q 2-3 min until response obtained; repeat q 1-2 hr if needed.

IV, IM, Subcut (Adults): Patients not suspected of being opioid dependent--0.4 mg (10 mcg/kg); may repeat q 2-3 min (IV route is preferred). Some patients may require up to 2 mg. Patients suspected to be opioid dependent--Initial dose should be decreased to 0.1-0.2 mg q 2-3 min.
Fentanyl - Indication
Management of breakthrough cancer pain in patients with malignancies who are already receiving and are tolerant to opioid therapy for their underlying cancer pain.
Fentanyl - Action
Binds to opiate receptors in the CNS, altering response to and perception of pain.
Fentanyl - Pharmacokinetics
Well absorbed (92% of dose) through skin surface under transdermal patch

Mostly metabolized by the liver 10-25% excreted unchanged by the kidneys.

Half-life: 17 hr after removal of a single application patch, increases to 21 hr after removal of multiple patches
Fentanyl - onset, peak, duration
Transdermal 6 hr† 12-24 hr 72 hr‡

Oral/transmucosal rapid 15-30 min several hrs
Fentanyl - adverse effects
CNS: confusion, sedation, weakness, dizziness, restlessness.
Resp: APNEA, bronchoconstriction, laryngospasm, respiratory depression.
CV: bradycardia.
GI: anorexia, constipation, dry mouth, nausea, vomiting.
Derm: sweating, erythema.
Local: application site reactions. MS: skeletal and thoracic muscle rigidity.
Misc: physical dependence, psychological dependence.
Fentanyl - route/dosage
Transdermal (Adults): 25 mcg/hr is the initial dose; patients who have not been receiving opioids should receive not more that 25 mcg/hr.

Morphine 10 mg IM or 60 mg PO q 4 hr (60 mg/24 hr IM or 360 mg/24 hr PO) is considered to be approximately equivalent to transdermal fentanyl 100 mcg/hr. Transdermal patch lasts 72 hr in most patients.