Diazepam / baclofen suppositories are a compounded, prescription preparation that is inserted vaginally or rectally. The most commonly ordered combination is diazepam 5 mg with baclofen 10 mg, molded into a suppository base and dispensed in a 15-count or 30-count. Some prescriptions also include ketamine. They are prepared by a licensed pharmacy to the strengths your prescriber orders rather than mass-produced.
Prescribers order them for hypertonic (high-tone) pelvic floor dysfunction, in which the muscles of the pelvic floor stay tight and can cause pelvic pain, painful intercourse, or urinary and bowel symptoms. There is no FDA-approved vaginal or rectal suppository of diazepam, baclofen, or any combination of them for this or any other purpose, so the dosage form itself is unapproved. This page exists so that you and your prescriber can see what is actually known, including the findings that do not support it.
How does it work?
Diazepam is a benzodiazepine. It positively modulates GABA-A receptors, which produces muscle relaxation, reduced anxiety, and sedation, largely through effects on the central nervous system. Baclofen is a GABA-B agonist that acts at the spinal cord to reduce spasticity. Ketamine, when a prescriber includes it, is an NMDA receptor antagonist added with the intent of addressing neuropathic pain.
The idea behind giving these vaginally or rectally is that the medication sits near the levator ani and obturator internus muscles and may help them relax. That is the reasoning, not a proven effect.
What is it used for?
Prescribers order these suppositories for hypertonic pelvic floor dysfunction, and for the symptoms that go with it, such as pelvic pain, painful intercourse, and vaginismus. They are usually intended as an adjunct to pelvic floor physical therapy, not as a treatment on their own.
Benefit is not established for any of these uses, and Bayview makes no claim that these suppositories relieve pelvic pain, vaginismus, or painful intercourse. Only a licensed prescriber can decide whether to try them. Bayview Pharmacy does not provide consultations and does not determine whether a medication is appropriate for you; a valid prescription is required.
What does the evidence show?
Plainly: benefit is not established, and the controlled trials that exist are negative.
- The main randomized trial found no benefit. Crisp and colleagues (Int Urogynecol J, 2013; N=21) compared nightly 10 mg vaginal diazepam with placebo over four weeks. There was no difference in resting vaginal EMG at any time point, and no difference on any validated questionnaire.
- A second placebo-controlled trial also found no benefit. A double-blind, placebo-controlled study published in Female Pelvic Medicine & Reconstructive Surgery in 2019 likewise failed to show an advantage over placebo.
- A 2025 systematic review found the evidence base small and low quality. That is the current state of the literature, not a pending question with a promising answer.
- Baclofen suppositories have no completed randomized trial. The support consists of case series and conference abstracts.
- Ketamine has no controlled evidence for this route or this indication.
- No society guideline endorses these. No urogynecology, urology, or gynecology society guideline recommends compounded diazepam or baclofen suppositories as standard therapy.
The honest bottom line is that pelvic floor physical therapy is the intervention with actual evidence for hypertonic pelvic floor dysfunction. If you are considering these suppositories, ask your prescriber how they fit alongside physical therapy rather than in place of it.
How is it used?
Use them exactly as your prescriber directs. As commonly prescribed, one suppository — often diazepam 5 mg with baclofen 10 mg — is inserted vaginally or rectally at bedtime, or twice daily, and dispensed in a 15-count or 30-count. Strengths seen in practice range from diazepam 2–10 mg with baclofen 5–20 mg.
Prescribers usually set a defined trial of two to four weeks, often timed around pelvic floor physical therapy sessions, rather than open-ended refills. Wash your hands before and after inserting. Because sedation is expected, bedtime dosing is common, and you should not drive or do anything requiring alertness until you know how it affects you. A panty liner can help with base leakage. These details describe common regimens and are not treatment recommendations; your prescriber sets the strengths, the schedule, and when to stop.
What strengths are made?
These suppositories are compounded to order. The combinations below are the ones prescribers request most often.
| Combination | Route | Count |
|---|---|---|
| Diazepam 5 mg / baclofen 10 mg | Vaginal or rectal | 15 or 30 |
| Diazepam 10 mg / baclofen 10 mg | Vaginal or rectal | 30 |
| Custom: diazepam 2–10 mg / baclofen 5–20 mg | Vaginal or rectal | As ordered |
| Diazepam / baclofen / ketamine (e.g. 5-5-17.25 mg to 5-5-25 mg) | Vaginal or rectal | 30 |
Strengths are listed for reference only. None has been shown to be better than placebo, and listing them is not a statement that any combination works or that one is better than another.
Side effects & safety
Expect sedation. Drowsiness, dizziness, impaired driving and coordination, falls, and problems with memory or concentration are the effects reported most often, and they are made worse by alcohol and by opioids. Do not drink alcohol while using these, and tell your prescriber about every medication you take, especially opioids, other sedatives, sleep medications, and muscle relaxants.
Extra caution is needed in older adults (benzodiazepines appear on the Beers criteria list of medications to avoid), and in people with breathing problems, sleep apnea, liver impairment, or a history of substance use.
Baclofen can cause drowsiness and muscle weakness. Stopping baclofen abruptly can cause a serious withdrawal syndrome with seizures, fever, confusion, muscle stiffness, and hallucinations, so it should be tapered rather than stopped suddenly, and doses need care in kidney impairment.
Local effects include vaginal irritation, discharge, and leakage or staining from the suppository base. Avoid use in pregnancy and while breastfeeding unless you have had a clear conversation with your prescriber about it.
Who should not use it?
Do not use these if you are allergic to diazepam, baclofen, ketamine (in versions containing it), or any ingredient in the suppository base. They are not appropriate if you have a benzodiazepine allergy, acute narrow-angle glaucoma, or severe respiratory insufficiency, and they should be avoided or used only with specific direction if you take opioids, have untreated sleep apnea, severe liver disease, myasthenia gravis, or a history of benzodiazepine or other substance misuse. Avoid in pregnancy and lactation absent a clear discussion with your prescriber. Tell your prescriber about your full health history, your allergies, and everything you take, including alcohol and anything bought over the counter.
How should it be stored?
Store them according to your label, because it depends on the base. Polyethylene glycol (PEG) based suppositories are generally kept at controlled room temperature. Cocoa butter and other fatty-base suppositories are generally refrigerated at 2–8 °C, or at least kept below 25 °C, so they do not melt. Follow the storage instruction the pharmacy puts on your label.
Protect them from light and heat, and do not store them in a bathroom. Because diazepam is a controlled substance, keep them secured and out of the reach of children and anyone else in the household, and do not share them. Discard after the beyond-use date on the label, and dispose of unused suppositories through a drug take-back program.
Why is this compounded?
There is no FDA-approved vaginal or rectal suppository of diazepam, baclofen, or any combination of them. The approved and commercially available products are oral diazepam tablets and solution (Valium), diazepam rectal gel (Diastat, approved only for acute repetitive seizures), oral baclofen and intrathecal baclofen (Lioresal), ketamine injection, and esketamine nasal spray (Spravato). A suppository can therefore exist only as a compounded preparation.
When a prescriber orders one, Bayview Pharmacy prepares it as a 503A compounding pharmacy under USP <795> standards, at the strengths and in the base specified. Compounding makes the dosage form available; it does not make it effective. Compounded preparations are not FDA-approved.
Clinical details for prescribers
Key negative evidence. Crisp CC, Vaccaro CM, Estanol MV, et al. Intra-vaginal diazepam for high-tone pelvic floor dysfunction: a randomized placebo-controlled trial. Int Urogynecol J. 2013;24(11):1915–23. N=21. Nightly vaginal diazepam 10 mg over 4 weeks produced no difference in resting vaginal EMG at any time point and no difference on any validated questionnaire versus placebo. A second double-blind placebo-controlled trial (Female Pelvic Med Reconstr Surg, 2019) also failed to demonstrate benefit over placebo. A 2025 systematic review concluded the evidence base is small and of low quality. Baclofen suppositories are supported only by case series and abstracts, with no completed RCT. Ketamine has no controlled evidence for this route or indication.
Bottom line. Benefit is not established. Pelvic floor physical therapy is the intervention with actual evidence for hypertonic pelvic floor dysfunction; suppositories are adjunctive at best. No urogynecology, urology, or gynecology society guideline endorses compounded diazepam or baclofen suppositories as standard therapy.
Pharmacokinetics. Vaginal diazepam is not confined locally — measurable serum concentrations occur after vaginal administration, so systemic benzodiazepine effects and interactions apply. Counseling that frames the route as “local only” or as having minimal systemic absorption is not accurate.
Regulatory. FDA-approved products: oral diazepam tablets/solution (Valium); diazepam rectal gel (Diastat, indicated only for acute repetitive seizures); oral baclofen and intrathecal baclofen (Lioresal); ketamine injection; esketamine nasal spray (Spravato). No FDA-approved vaginal or rectal suppository of diazepam, baclofen, or any combination exists for pelvic floor dysfunction — the dosage form itself is unapproved. Diazepam is a Schedule IV controlled substance; DEA registration and CIV prescribing, recordkeeping, and refill limits apply. FDA issued a warning on October 10, 2023 regarding compounded ketamine products (sedation, dissociation, worsening psychiatric symptoms, blood pressure elevation, respiratory depression, abuse and misuse, lower urinary tract and bladder toxicity), specifically addressing unmonitored at-home use. Compounded preparations are not FDA-approved.
Formulation & SIG. Commonly diazepam 5 mg / baclofen 10 mg vaginal or rectal suppository; also diazepam 10 mg / baclofen 10 mg; custom diazepam 2–10 mg with baclofen 5–20 mg; ketamine-containing versions (e.g. 5-5-17.25 mg to 5-5-25 mg). Dispensed 15 or 30 count. Descriptive SIG: insert one suppository vaginally or rectally at bedtime, or twice daily. Prepared under USP <795>.
Clinical points:
- Set a defined trial duration (commonly 2–4 weeks) with a stop or taper plan rather than open-ended refills; consider timing around pelvic floor physical therapy sessions.
- Monitor sedation, functional impairment, cumulative benzodiazepine exposure, and signs of dependence; counsel on driving, alcohol, and concurrent opioids.
- Reassess with pelvic floor examination and validated pain and function measures rather than refill volume.
- Benzodiazepine boxed warnings apply: risks from concomitant opioid use (profound sedation, respiratory depression, coma, death); abuse, misuse, and addiction; dependence and withdrawal reactions, including seizures, on abrupt discontinuation.
- Baclofen requires tapering; abrupt withdrawal can cause seizures, fever, confusion, muscle rigidity, and hallucinations. Reduce dose in renal impairment.
- Caution in older adults (Beers criteria), respiratory disease, sleep apnea, hepatic impairment, and substance use history. Avoid in pregnancy and lactation absent a clear risk discussion.
- Comply with DEA Schedule IV prescribing, recordkeeping, and refill limitations; a DEA number is required.
Ordering: e-prescribe to Bayview. Bayview does not recommend this preparation and makes no efficacy claim; it is prepared on prescriber request as an adjunct within a prescriber-directed plan. References: Crisp et al., Int Urogynecol J 2013; FDA compounded ketamine warning (October 10, 2023).
This is a prescription compounded medication and is not FDA-approved. This information is educational and is not medical advice, and it is not a recommendation to use this preparation. Benefit for hypertonic pelvic floor dysfunction, pelvic pain, vaginismus, and painful intercourse is not established; randomized placebo-controlled trials of vaginal diazepam were negative, and pelvic floor physical therapy is the intervention with actual evidence. Diazepam is a Schedule IV controlled substance. Your prescriber determines whether it is appropriate and sets the strengths and directions. A valid prescription is required.
