Names and pronunciation
(dye-az′-e-pam) Diastat, Dio-Stat Acudial, Valium, Valtoco
Source page 382
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Individual generic drug information
Extracted information for diazePAM only.
(dye-az′-e-pam) Diastat, Dio-Stat Acudial, Valium, Valtoco
Source page 382
Func. class.: Antianxiety, anticonvulsant, skeletal muscle relaxant, central acting
Source page 382
Chem. class.: Benzodiazepine, long-acting Controlled Substance Schedule IV
Source page 382
Do not confuse: diazePAM/Ditropan/LORazepam
Source page 382
ACTION: Potentiates the actions of GABA, especially in the limbic system, reticular formation; enhances presympa- thetic inhibition, inhibits spinal polysyn- aptic afferent paths
Source page 382
USES: Anxiety, acute alcohol with- drawal, adjunct for seizure disorders; preoperatively as a relaxant for skeletal muscle relaxation; rectally for acute repetitive seizures
Source page 382
Extracted information for diazePAM only.
CONTRAINDICATIONS: Preg- nancy, hypersensitivity to benzodiaze- pines, closed-angle glaucoma, coma, myasthenia gravis, ethanol intoxication, hepatic disease, sleep apnea Precautions: Breastfeeding, children <6 mo, geriatric patients, debilitation, renal disease, asthma, bipolar disorder, COPD, CNS depression, labor, Parkin- son’s disease, neutropenia, psychosis, seizures, substance abuse, smoking
Source page 382
Black Box Warning: Coadministration with other CNS depressants, respiratory depression Black Box Warning: Avoid coadministra- tion with other CNS depressants; do not use with opioids Black Box Warning: Respiratory de- pression: monitor for respiratory depres- sion, respirations q5-15 min if given IV • IV site for thrombosis or phlebitis, which may occur rapidly • Mental status: mood, sensorium, af- fect, sleeping pattern, drowsiness, dizzi- ness, suicidal tendencies • Physical dependency, withdrawal symptoms: headache, nausea, vomiting, muscle pain, weakness after long-term, high-dose use • Beers: avoid use in older adults; may be appropriate for seizures, sleep disor- ders, benzodiazepine/ethanol with- drawal, severe anxiety disorders • Pregnancy/breastfeeding: use in pregnancy not recommended; do not breastfeed, excretion in breast milk
Source pages 383, 384
SIDE EFFECTS CNS: Dizziness, drowsiness, headache, hangover, slurred speech, paradoxical excitation CV: Hypotension, tachycardia EENT: Blurred vision GI: Constipation, nausea, vomiting, diar- rhea, weight gain INTEG: Rash, dermatitis, itching, phlebi- tis (IV), venous thrombosis RESP: Respiratory depression MISC: Psychological/physical depen- dency, tolerance, neutropenia
Source pages 383, 384
INTERACTIONS Increase: diazepam effect—amiodarone, protease inhibitors, dilTIAZem, cimeti- dine, clarithromycin, dalfopristin-quinu- pristin, delavirdine, disulfiram, efavirenz, erythromycin, fluconazole, fluvoxaMINE, imatinib, itraconazole, ketoconazole, IV miconazole, nefazodone, niCARdipine, ranolazine, troleandomycin, valproic acid, verapamil, voriconazole, zafirlu- kast, zileuton; monitor for increased sedation Increase: toxicity—barbiturates, SSRIs, cimetidine, CNS depressants, valproic acid, CYP3A4 inhibitors Increase: CNS depression—CNS depres- sants, alcohol; monitor for increased sedation Decrease: diazePAM metabolism—oral contraceptives, valproic acid, disulfiram, isoniazid, propranolol Decrease: diazePAM effect—CYP3A4 inducers (rifAMPin, barbiturates, carBA- Mazepine, ethotoin, phenytoin, fosphe- nytoin), smoking Drug/Herb Increase: CNS depression—kava, cham- omile, valerian Drug/Lab Test Increase: AST/ALT, alkaline phosphatase
Source page 384
TREATMENT OF OVERDOSE: Lavage, VS, supportive care, flumazenil See Appendix B
Source page 385
Extracted information for diazePAM only.
DOSAGE AND ROUTES Anxiety/seizure disorders • Adult: PO 2-10 mg bid-qid; IM/IV 2-5 mg q3-4hr • Geriatric: PO 2-2.5 mg daily-bid, in- crease slowly as needed • Child >6 mo: PO 1-2.5 mg tid/qid; IM/IV 0.04-0.3 mg/kg/dose q2-4hr, max 0.6 mg/kg in an 8-hr period Precardioversion • Adult: IV 5-15 mg 5-10 min precar- dioversion Preendoscopy • Adult: IV 2.5-20 mg; IM 5-10 mg ½ hr preendoscopy Muscle relaxation • Adult: PO 2-10 mg tid-qid or EX- TENDED RELEASE 15-30 mg/day; IV/IM 5-10 mg, repeat in 2-4 hr Tetanic muscle spasms • Adult: IV/IM 10 mg, then 10 mg in 3-4 hr • Child >5 yr: IM/IV 5-10 mg q3-4hr prn • Infant >30 days: IM/IV 1-2 mg q3- 4hr prn Status epilepticus • Adult: IV/IM 5-10 mg, 2 mg/min, may repeat q10-15min, max 30 mg; may re- peat in 2-4 hr if seizures reappear • Child >5 yr: IM 1 mg q2-5min; IV 1 mg slowly • Child 1 mo-5 yr: IV 0.2-0.5 mg slowly; IM 0.2-0.5 mg slowly q2-5min up to 5 mg, may repeat in 2-4 hr prn Seizures other than status epilepticus • Adult: RECT 0.2 mg/kg, may repeat in 4-12 hr • Child 6-11 yr: RECT 0.3 mg/kg, may repeat in 4-12 hr • Child 2-5 yr: RECT 0.5 mg/kg, may repeat in 4-12 hr Alcohol withdrawal • Adult: IV 10 mg initially, then 5-10 mg q3-4hr prn Psychoneurotic reactions • Adult: IM/IV 2-10 mg, may repeat in 3-4 hr Epilepsy cluster seizures Adult: Nasal spray 0.2 mg/kg or 0.3 mg/kg, depending on the patient’s age and weight
Source page 383
Available forms: Tablets 2, 5, 10 mg; injec- tion 5 mg/mL; oral solution 5 mg/5 mL, rectal 2.5 (pediatric), 10, 20 mg, twin packs; extended-release capsule 15 mg, rectal gel; D nasal spray 5 mg in 0.1 mL
Source page 383
Administer: PO route • With food or milk for GI symptoms; crushed if patient is unable to swallow medication whole • Reduce opioid dose by 1⁄3 if given concomitantly with diazepam • Concentrate: use calibrated dropper only; mix with water, juice, pudding, ap- plesauce; to be consumed immediately Rectal route • Do not use more than 5×/mo or for an episode q5days (Diastat) Nasal route • Do not prime • Place patient on side or back • Remove from blister pack • Insert nozzle in nostril, press plunger to deliver dose, remove IM route • Painful, use deltoid if used this route Direct IV route • Have emergency equipment nearby • Observe for several hours after IV; if used in combination with opioids, de- crease opioid dose • Into large vein; give IV 5 mg or less/1 min or total dose over 3 min or more (children, infants); continuous infusion is not recommended; inject as close to vein insertion as possible; do not dilute or mix with other products
Source page 383
Extracted information for diazePAM only.
Assess: • CV: B/P (lying, standing), pulse; if systolic B/P drops 20 mm Hg, hold prod- uct, notify prescriber • Blood studies: CBC during long-term therapy; blood dyscrasias (rare); hepatic studies: AST, ALT, bilirubin, creatinine, LDH, alkaline phosphatase • IV site: frequently, watch for phlebitis • Degree of anxiety: what precipitates anxiety and whether product controls symptoms • Alcohol withdrawal symptoms, in- cluding hallucinations (visual, auditory), delirium, irritability, agitation, fine to coarse tremors • Seizure control and type, duration, in- tensity of seizures • For muscle spasms; pain relief
Source page 384
Evaluate: • Therapeutic response: decreased anxiety, restlessness, insomnia
Source page 384
CLINICAL CONSIDERATIONS
Source page 384
Patient and caregiver information: • That product may be taken with food • That product not to be used for every- day stress or for >4 mo unless directed by prescriber; to take no more than pre- scribed amount; that product may be habit forming, review package insert with patient • To avoid OTC preparations unless ap- proved by prescriber • To avoid driving, activities that require alertness; drowsiness may occur • To avoid alcohol, other psychotro- pic medications unless directed by prescriber; that smoking may decrease diazePAM effect by increasing diaze- PAM metabolism • Not to discontinue medication abruptly after long-term use; to gradually taper • To rise slowly or fainting may occur, especially in geriatric patients • That drowsiness may worsen at begin- ning of treatment • To notify prescriber if pregnancy is planned or suspected; to avoid breastfeeding
Source pages 384, 385
Extracted information for diazePAM only.
PHARMACOKINETICS Metabolized by liver via CYP2C19, CYP3A4; 15%-20% of Asian patients and up to 5% of White and Black patients are poor metabolizers; excreted by kid- neys; crosses placenta; excreted in breast milk; crosses the blood-brain barrier; half-life 1-12 days; more reliable by mouth; 99% protein binding PO: Rapidly absorbed, onset ½ hr, peak 2 hr, duration up to 24 hr IM: Onset 15-30 min, duration 1-1½ hr, absorption slow and erratic RECT: Peak 1.5 hr IV: Onset immediate, duration 15 min-1 hr
Source page 384
Filter the extracted dose blocks for this individual drug.
Anxiety/seizure disorders
• Adult: PO 2-10 mg bid-qid; IM/IV 2-5 mg q3-4hr
Candidate age grouping · source page 383
Anxiety/seizure disorders
• Geriatric: PO 2-2.5 mg daily-bid, in- crease slowly as needed
Candidate age grouping · source page 383
Anxiety/seizure disorders
• Child >6 mo: PO 1-2.5 mg tid/qid; IM/IV 0.04-0.3 mg/kg/dose q2-4hr, max 0.6 mg/kg in an 8-hr period Precardioversion
Candidate age grouping · source page 383
Anxiety/seizure disorders
• Adult: IV 5-15 mg 5-10 min precar- dioversion Preendoscopy
Candidate age grouping · source page 383
Anxiety/seizure disorders
• Adult: IV 2.5-20 mg; IM 5-10 mg ½ hr preendoscopy Muscle relaxation
Candidate age grouping · source page 383
Anxiety/seizure disorders
• Adult: PO 2-10 mg tid-qid or EX- TENDED RELEASE 15-30 mg/day; IV/IM 5-10 mg, repeat in 2-4 hr Tetanic muscle spasms
Candidate age grouping · source page 383
Anxiety/seizure disorders
• Adult: IV/IM 10 mg, then 10 mg in 3-4 hr
Candidate age grouping · source page 383
Anxiety/seizure disorders
• Child >5 yr: IM/IV 5-10 mg q3-4hr prn
Candidate age grouping · source page 383
Anxiety/seizure disorders
• Infant >30 days: IM/IV 1-2 mg q3- 4hr prn Status epilepticus
Candidate age grouping · source page 383
Anxiety/seizure disorders
• Adult: IV/IM 5-10 mg, 2 mg/min, may repeat q10-15min, max 30 mg; may re- peat in 2-4 hr if seizures reappear
Candidate age grouping · source page 383
Anxiety/seizure disorders
• Child >5 yr: IM 1 mg q2-5min; IV 1 mg slowly
Candidate age grouping · source page 383
Anxiety/seizure disorders
• Child 1 mo-5 yr: IV 0.2-0.5 mg slowly; IM 0.2-0.5 mg slowly q2-5min up to 5 mg, may repeat in 2-4 hr prn Seizures other than status epilepticus
Candidate age grouping · source page 383
Anxiety/seizure disorders
• Adult: RECT 0.2 mg/kg, may repeat in 4-12 hr
Candidate age grouping · source page 383
Anxiety/seizure disorders
• Child 6-11 yr: RECT 0.3 mg/kg, may repeat in 4-12 hr
Candidate age grouping · source page 383
Anxiety/seizure disorders
• Child 2-5 yr: RECT 0.5 mg/kg, may repeat in 4-12 hr Alcohol withdrawal
Candidate age grouping · source page 383
Anxiety/seizure disorders
• Adult: IV 10 mg initially, then 5-10 mg q3-4hr prn Psychoneurotic reactions
Candidate age grouping · source page 383
Anxiety/seizure disorders
• Adult: IM/IV 2-10 mg, may repeat in 3-4 hr Epilepsy cluster seizures Adult: Nasal spray 0.2 mg/kg or 0.3 mg/kg, depending on the patient’s age and weight
Candidate age grouping · source page 383