ALPRAZOLAM (XANAX)

CLASSIFICATION: CENTRAL NERVOUS SYSTEM AGENT; ANXIOLYTIC; SEDATIVE-HYPNOTIC; BENZIODIAZEPINE

PROTOTYPE: Lorazepam
Pregnancy Category: D
Controlled substance: Scheduled IV

Availability: 0.25mg, 0.5mg, 1mg, 2mg tablets; 0.5mg/5mL, 1mg/mL oral solution.

Actions: CNS depressant. Mode of action not known, thalamic, and hypothalamic levels of the CNS. It is associated with significantly less drowsiness.

Therapeutic Effect: Drug has antidepressant as well as antianxiety actions.

Uses: Management of anxiety disorder of for short-term relief of anxiety symptoms. Also used as adjunct in management of anxiety associated with depression and agitation and for panic disorders, such as agoraphobia.

Contraindications: Sensitive to benzodiazepines; acute narrow angle glaucoma; pulmonary disease; use alone in primary depression or psychotic disorders; during pregnancy (category D), lactation and children <18y.

Cautious Use: Impaired renal or hepatic function; history of alcoholism; geriatric and debilitated patients.Effectiveness for long term treatment (>4 mo.) not established.

Route and Dosage:

Anxiety Disorder:
Adult: PO 0.25-0.5 mg t.i.d. (max: 4mg/d)
Geriatric: PO 0.125-0.25 mg b.i.d.

Panic Attack:
Adult: PO 1-2mg t.i.d. (max: 8mg/d)


ADMINISTRATION
 Oral:

• Reduce drug gradually when discontinuing drug.
• Store in light-resistant containers at 15-30degrees C (59-86deg. F), unless otherwise directed.

Adverse Effect: (>_1%)
CNS: Drowsiness, sedation, light-headedness, dizziness, syncope, depression, headache, confusion, insomnia, nervousness, fatigue, clumsiness, unsteadiness, rigidity, tremor, restlessness, paradoxical excitement, hallucinations.
CV: Tachycardia, hypotension, ECG changes.
Special Senses: Blurred vision.
Respiratory: dyspnea.

INTERACTION Drug: Alcohol and other CNS DEPRESSANTS, ANTICONVULSANTS, ANTIHISTAMINES, BARBITURATES, NARCOTIC ANALGESICS, BENZODIAZEPINES compound CNS depressant effects;
Herbal: Kava-kava, valerian may potentiate sedation.

PHARMACOKINETICS:
Absorption: Rapidly absorbed.
Peak: 1-2h.
Distribution: Crosses placenta.
Metabolism: Oxidized in liver to inactive metabolities.
Elimination: Renal elimination.
Half-Life: 12-15h,

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CARISOPRODOL (SOMA)

CLASSIFICATIONS: Autonomic Nervous System Agent; Skeletal Muscular Relaxant: Central-Acting

PROTOTYPE: Cyclobenzaprine

PREGNANCY CATEGORY: C

AVAILABILITY: 350mg tablets

ACTIONS: Propanediol derivative carbamate with cantral depressant action pharmacologically related to meprobamate. Precise action mechanism of CNS depression is not clear. Skeletal muscle relaxant effect, unlike that of neuromuscular blocking agents, appears to be due to sedative action. Voluntary motor function is not lost, but there may be slight reduction in muscle tone leading to relief of pain and discomfort of muscle spasm.

THERAPUTIC EFFECTS: Effective spasmolytic and reduces pain asociated with acute musculoskeletal disorders.

USES: Skeletal muscular spasm, stiffness, and pain in a variety of musculoskeletal disorders and to relieve spasticity and rigidity in cerebral palsy.

CONTRAINDICATION: Hypersensitivity to carisoprodol and related compounds (e.g., meprobamate, tybamate); acute intermittent porphyria; children <5y; pregnancy (category C), lactation.

CAUTIOUS USE: Impaired liver or kidney function, addiction-prone individuals.

ROUTE AND DOSAGE:
MUSCLE SPASM:
Adult: PO 350 mg t.i.d.
Child: PO >5y, 25mg/kg/d in
4 divided doses

ADMINISTRATION:
Oral:

• Give with food, as needed, to reduce GI symptoms. Last dose should be taken at bedtime.
• Store in tightly closed container

ADVERSE EFFECTS (>-1%) Body as a whole: Eosinophilia, asthma, fever, anaphylactic shock.

CV: Tachycardia, postural hypotension, facial flushing.

GI: Nausea, vomiting, hiccups.

CNS: Drowsiness, dizzeness, vertigo, ataxia, tremor, headache, irritability, depressive reactions, syncope, insomia.

SKIN: skin rash, erythema multiforme, pruritus.

INTERACTIONS Drug: Alcohol, CNS depressants potentiate CNS effects.

PHARMACOKINETICS Onset: 30min.

Duration: 4-6h.

Distribution: crosses placenta.

Metabolism: Metabolized in liver.

Elimination: Excreted by kidneys; excreted in breast milk (2-4 times the plasma concentrations).

Half Life: 8h.

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TRAMADOL HYDROCHRORIDE (Tramadol)

Ultram, Zydol
Classification: Central nervous system agent, opiate agonist; Narcotic Analgesic
Prototype: Morphine sulfate
Pregnacy Type: C

Availability: 50mg tablets

Actions: Centrally acting opiate receptor agonist that inhibits the uptake of norepinephrine and serotonin, suggesting both opioid and nonoptioid mechanism of pain relief. May produce opoiod-like effects, but causes less respiratory depression than morphine.

Theraputic Effects:
Effective agent for control of moderate to moderate severe pain.

Use: Management of moderate to moderately severe pain.

Contraindication: Hypersensitivity to tramadol or other opoiod analgesics: patients in MAO inhibitors; patients acutely intoxicated with alcohol, hypnotics, centrally acting analgesics, opoiods, or psyctropic drugs; patients on obstretric preoperative medication; lactation.

Cautious Use: Debilitated patients; chronic respiratory disorders; Liver disease; renal impairment; myxedema, hypothyroidism, or hypoadrenalism; acute abdominal conditions; increased ICP or head injury; history of siezures; pregnancy (category C); patients >75y. Safely and efficacy i children are not established.

Route and Dosage:
Pain
Adult: PO 50-100mg q4-6h prn(max: 400mg/d), may start with 25mg/d if not well tolerated, and increase by 25mg q3d up to 200mg/d
Geriatric:PO 50-100mg q4-6h prn (max:300mg/d), may start with 25mg/d if not well tolerated, and increase by 25 mg q3d up to 200mg/d

Renal Impairment:
Clcr <30mL/min: decrease to 50-100mg q 12h
Hepatic Impairment cirrhosis decrease to 50-100 mg q12h.

Administration:
Oral
Note: Dosage reduction is recomended for patients with renal insufficientcy and hepatic impairment.
Store at 15 to 30degrees C (59 to 86degrees F).

Adverse Effects: CNS: Drowsiness, dizziness, vertigo, fatigue, headache, somnolence, restlessness. euphoria, confusion, anxiety, coordination disturbance, sleep disturbances, siezures. CV: palpitations, vasodilation. GI: Nausea, constipation, vomiting, xerostomia, dyspepsia, diarrhea, abdominal pain, anorexia, flatylence. Body as a Whole: Sweating, anaphylactics reaction (even with first dose).
Skin: Rash Special senses: Visual disturbances. Urogenital: Urinary retention/frequency, menopausal symptoms.

Diagnostic Test Interference: Increased creatinine, liver enzymes; decreased hemoglobin; protienuria.


Interactions Drug: Carbamazepine significantly decreases tramadol level (may need up to twice usual dose). Tramadol may increase adverse effects of MAO INHIBITORS. TRICYCLIC ANTIDEPRESANTS, cyclobenzaprine, PHENOTHIAZINES, SELECTIVE SEROTONIN-REUPTAKE INHIBITORS (SSRIS), MAO INHIBITORS may enhance seizure risk with tramadol. May increase CNS adverse effects when used with other CNS DEPRESANTS. Herbal: St. John's Wort may increase sedation.

PHARMACOKINETICS Absorption:
Rapidly absorbed from GI tract; 75% reaches systemic circulation.
Onset: 30-60 min.
Peak: 2h
Duration: 3-7hrs
Distribution: Approximately 20% bound to plasma proteins; probably crosses blood-brain barrier; crosses placenta; 0.1% excreted into breast milk.
Metabolism: Metabolized extensively in liver by cytocrome P450 system.
Elimination: Excreted primarily in urine.
Half Life: 6-7h.

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ABACAVIR SULFATE (ZIAGEN)

Classification:
Antiinfection, Antiviral, Antiretroviral agent; Nucleoside Reverse Transcriptase Inhibitor (NRTI)

Prototype: Zidovudine
Pregnancy Caterogy: C

Availability 300 mg tablets; 20mg mL oral solution

Actions:
Abacavir is a synthetic nucleoside analogue with inhibitory activity against HIV. It inhibit the activity of HIV-1 Reverse Transcriptase (RT) both by completing with the natural DNA nucleoside and by incorporation into viral DNA.

Theraputic Effects:
Abacavir prevents the formation of viral DNA replication. Therefore the viral load decreases as measured by an increased CD4 lymphocyte cell count and suppression of HIV RNA, indicated by decreases HIV RNA copies, in HIV-positive individuals with little or no exposure to zidovudine (AZT).

Uses:
Treatment of HIV infection in combination with other anti retroviral agents.

Contraindications:
Hypersensitivity to avacavir; pregnancy (category C); lactation.

Cautious Use:
Prior resistance to another Nucleoside Reverse Transcriptase Inhibitor (NRTI); hepatic dysfunction; older adults.

Route & Dosage:
HIV Infection:
Adult: PO 300mg b.i.d.
Child: PO 3mo-16y, 8mg/kg b.i.d. (max: 300mg b.i.d.)

Administration:
Oral

• Tablets & Oral solution are interchangeable on a mg-for-mg basis.
• Store tables and liquid at 20degree-25degree C (68-77degree F). Liquid maybe refrigerated.

Adverse Effect:
Body as a whole: Hypersensitivity reactions (including fever, skin rash, fatigue, nausea, vomiting, diarrhea, abdominal pain); malaise: lethargy; myalgia; arthralgia; parenthesia; edema; shortness of breath. CNS: Insomnia, headache, fever. CV: Hypotension (associated with hypersensitivity reaction). GI: Hepatomegaly with stenosis, nausea, vomiting, diarrhea, anorexia, panceatitis, increased GGT, increased liver function test. Skin: rash. Other: Lactic acidosis, renal insuficiency

Pharmacokinetics Absorption:
Rapidly absorbed, 83% bioavailable.
Distribution: Distribute into extravascular space and erythrocytes; 50% protein bound.
Metabolism: Metabolozed by alcohol dehydrogenase and glucuronyl transferase to inactive metabolites.
Elimination: 84% excreted in urine, primary as inactive metabolites; 16% excreted in feces.
Half life: 1.5 h

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