Diazepam

Selected oral labels cover anxiety disorders / short-term symptom relief, acute alcohol-withdrawal symptoms, adjunctive skeletal muscle spasm/spasticity and adjunctive convulsive-disorder treatment. Everyday stress usually does not need an anxiolytic; oral diazepam is not established as sole seizure therapy, and usefulness beyond 4 months requires periodic reassessment. Injection additionally covers adjunctive status epilepticus/severe recurrent seizures, tetanus, endoscopic/surgical premedication and cardioversion-related anxiety/amnesia.

Valtoco and selected rectal gel treat identifiable intermittent seizure clusters distinct from the usual pattern in patients with epilepsy ≥2. Neither is a chronic daily antiseizure regimen or a substitute for the established maintenance treatment/emergency plan. Caregivers must recognize the correct episode, administer the exact product and identify when professional rescue is needed.

Standard oral solution 5 mg/5 mL is 1 mg/mL; Intensol 25 mg/5 mL is 5 mg/mL, fivefold more concentrated. Verify prescribed mg and mL with the pharmacist. Intensol uses only its supplied calibrated oral syringe; mix a single dose into liquid or soft food, consume the entire mixture immediately and do not save it. After continued use, use a patient-specific gradual taper; pause or slow the taper if withdrawal develops under prescriber direction. No universal taper decrement or duration is supplied.

Selected pediatric status regimen ages 3 months through 17: first 0.2 mg/kg, maximum 8 mg, slow IV push over 1 minute; if necessary a second 0.1 mg/kg, maximum 4 mg, 5 minutes after the first, also over 1 minute. For tetanus above 30 days, label describes 1–2 mg IM/slow IV every 3–4 hours as needed; at ≥5 years, 5–10 mg every 3–4 hours may be required. Do not extrapolate these indications to a universal pediatric dose. Respiratory assistance must be available. Other IV indications use at least 1 minute per 5 mg (5 mg/mL), avoiding small veins, intra-arterial administration and extravasation. Do not mix/dilute in syringe or infusion container; deep IM when indicated. Injection is not long-term seizure maintenance.

Selected rectal label uses age 2–5: 0.5 mg/kg; 6–11: 0.3 mg/kg; ≥12: 0.2 mg/kg, rounded upward to the next available labeled dose using its exact age/weight chart. Available selected doses are 5, 7.5, 10, 12.5, 15, 17.5 and 20 mg; pharmacist sets/locks the applicator to the prescribed dose. The chart is not identical to Valtoco; use the linked rectal label rather than copying nasal bands. If prescribed, a second rectal dose is 4–12 hours after first. Treat no more than 1 episode every 5 days or 5/month. Reassess dose with age/weight changes; older/debilitated patients may need a lower dose. Verify correct visible dose, locked collar and green READY marking before use; do not reuse. Remain with the person for 4 hours after treatment per selected caregiver instructions.

Oral selected labels contraindicate diazepam hypersensitivity, age <6 months, myasthenia gravis, severe respiratory/hepatic insufficiency, sleep apnea and acute narrow-angle glaucoma. Injection contraindicates hypersensitivity, acute narrow-angle glaucoma and open-angle glaucoma without appropriate treatment. Nasal/rectal labels contraindicate hypersensitivity and acute narrow-angle glaucoma; open-angle disease requires appropriate therapy. Do not transplant every oral contraindication as a formal contraindication of all routes; high-risk disease still needs individualized review.

All selected products carry boxed warnings for potentially fatal opioid coadministration; abuse, misuse and addiction; and dependence / withdrawal reactions. Reserve opioid combinations for inadequate alternatives, minimize exposure and monitor breathing/sedation. Gradual discontinuation is necessary after regular or excessive-frequency use; an intermittent rescue label does not permit unrestricted dosing.

Common reactions include drowsiness, fatigue, weakness and ataxia; injection adds local venous injury and nasal treatment local discomfort, taste change, bleeding or runny nose. Serious respiratory / cardiovascular collapse, paradoxical behavior, falls and dependence can occur. Overdose can progress from sleepiness / confusion to coma and respiratory depression, especially with alcohol/opioids. Obtain emergency/Poison Help assessment and professional airway support. Flumazenil can provoke seizures/withdrawal and is contraindicated after benzodiazepine treatment of a potentially life-threatening condition such as status epilepticus; its complete label requires review, not home use.

Opioids, alcohol, sedative antihistamines, anesthetics, antipsychotics, barbiturates and other sedatives can amplify sedation / respiratory effects. Minimize combinations and monitor; injection procedures require clinician-selected adjustments of companion narcotics. Valproate may increase CNS depression. Avoid independent substitution with another benzodiazepine or compensatory extra rescue doses.

CYP2C19/CYP3A4 inhibitors can prolong diazepam effects; examples in selected labels include cimetidine, ketoconazole, fluvoxamine, fluoxetine and omeprazole. Inducers such as rifampin, carbamazepine, phenytoin or phenobarbital may reduce rescue efficacy. Diazepam can slow phenytoin elimination, and possible interactions with other CYP substrates need review. Antacids may delay/lower oral peak without changing total absorption. No universal percentage dose adjustment or route-equivalence formula is supplied.

Use cautious lower starts in older/debilitated patients because diazepam / metabolites accumulate and increase ataxia, sedation and falls. Renal impairment can accumulate metabolites; selected nasal/rectal PK data in renal disease are lacking. Liver disease can markedly prolong elimination; severe hepatic insufficiency is an oral contraindication and lesser disease needs caution. No universal CrCl, Child-Pugh or dialysis dose formula is established for all routes.

Oral use below 6 months is contraindicated. Nasal/rectal cluster rescue is labeled at ≥2; unlisted weight bands require review. The selected IV status regimen is for 3 months–17 years; neonatal parenteral safety / effectiveness ≤30 days is unestablished and prolonged CNS depression / benzyl-alcohol harm is a concern. Indication-specific tetanus dosing above 30 days does not establish infant seizure dosing.

Individualize treatment during pregnancy; newer selected liquid, injection, nasal and rectal labels report no clear birth-defect association in observational studies, without guaranteeing safety, whereas the older Valium PI describes suggested malformation risk. Late pregnancy/labor exposure can cause neonatal hypotonia, respiratory/feeding problems or withdrawal requiring observation. Pregnancy registries are available. Diazepam appears in milk: selected regular oral labels advise against breastfeeding; injection/nasal labels weigh benefits/risks and monitor infant sedation, feeding and weight. Rectal label additionally advises an appropriate post-dose breastfeeding interval without specifying a universal number of hours. Obtain a product-specific feeding plan.

Diazepam enhances GABAergic inhibition through the benzodiazepine site of GABA-A receptors. This contributes to anxiolytic, sedative, anticonvulsant, muscle-relaxing and amnestic effects; the exact clinical antiseizure mechanism is not fully understood.

Oral

Peak usually about 1–1.5 hours; food delays absorption. Terminal half-life up to 48 hours; desmethyldiazepam up to 100 hours. Multiple dosing accumulates.

Nasal Valtoco

Adult peak about 1.5 hours, bioavailability about 97% versus IV; mean half-life about 49 hours after 10 mg.

Rectal gel

Adult peak about 1.5 hours, bioavailability about 90% versus injectable; mean parent/metabolite half-lives about 46/71 hours after 15 mg.

Metabolism / elimination

CYP2C19 and CYP3A4 produce active desmethyldiazepam, temazepam and oxazepam; conjugated metabolites mainly excreted in urine. Highly protein-bound.

Scope

Rapid IV redistribution, age/organ impairment and route affect response. These PK values do not validate dose interchange or a waiting period before emergency help.

Assess indication response, continued need, breathing, sedation, BP/falls, mood/paradoxical behavior, adherence and substance-use / dependence risk. Injection requires respiratory / cardiovascular monitoring and resuscitation readiness. Review renal/hepatic function when risk warrants; selected oral/injection labels advise periodic CBC and liver testing during long-term use. Rescue monitoring includes episode timing, breathing/color, response and total frequency; do not infer a routine lab panel or follow-up interval for all routes.

Avoid alcohol, sharing doses and driving until effects resolve and condition permits; store securely. Do not abruptly stop regular diazepam. Verify liquid concentration with a calibrated measure. For Valtoco never prime or test; one spray for 5/10 mg, one spray in each nostril for 15/20 mg. Follow the exact action plan, record dose times and seek emergency help for unusual/persistent seizures, alarming breathing/color or excessive sedation. Do not give a second nasal dose with concerning breathing/sedation. Rectal caregivers must verify the pharmacy-locked dose/READY marker, use the package instructions and remain with the person for 4 hours. Discuss pregnancy / breastfeeding and every new medicine.

Ingredient / route

Diazepam 2 mg · oral tablet.

Appearance / imprint

White scored round tablet with V-shaped perforation; 2 VALIUM / ROCHE.

Example NDC

0140-0004-01 · 100 tablets; selected Roche-distributed label.

U.S. status

Prescription benzodiazepine, DEA Schedule IV. Current source record is not a pharmacy-stock guarantee.

Oral tablets

Valium 2 mg white, 5 mg yellow and 10 mg blue; brand / strength-specific markings.

Oral liquids

Hikma standard 5 mg/5 mL (1 mg/mL); Intensol 25 mg/5 mL (5 mg/mL), contains 19% alcohol and supplies a calibrated oral syringe.

Injection

Selected Hospira 5 mg/mL, 50 mg/10 mL multidose vial; IM/IV only, not nasal/rectal.

Valtoco

5, 7.5 or 10 mg per 0.1 mL single-use device; packaged total doses 5/10/15/20 mg. The 15/20 mg dose uses TWO devices.

Rectal gel

Selected 10 mg delivery system sets 5/7.5/10 mg; 20 mg system sets 12.5/15/17.5/20 mg. These package names are not necessarily the prescribed dose.

Scope

Other branded rectal systems, compounded liquids and non-U.S. products require their exact labels; no cross-route substitution.

Valium 15–30°C in tight light-resistant container. Selected liquids and injection 20–25°C; protect from light, and use tight light-resistant liquid containers. Intensol: discard opened bottle after 90 days; consume mixed dose immediately. Valtoco 20–25°C (15–30°C excursions), no freezing, protect light and keep blister sealed until use; do not test devices. Rectal gel 25°C (15–30°C excursions); retain locked syringes and caregiver instructions. Keep all formulations securely away from children and others; pharmacist guidance for controlled-drug disposal.