Dosing & Uses
Dosage Forms & Strengths
anorectal cream
- 4% (H-Releve Hemorrhoidal)
- 5% (RectiCare, LMX5, Dr. Numb)
anorectal gel
- 5% (Topicaine 5)
Hemorrhoids or Anorectal Pain
Indicated for pain, itching, and burning associated with hemorrhoids and other anorectal disorders
Apply to perianal region up to 6 times/day
Not to be used inside the rectum
Administration
Not to be used inside the rectum
When practical, clean area with soap and water, and gently pat dry before use
Dosage Forms & Strengths
anorectal cream
- 4% (H-Releve Hemorrhoidal)
- 5% (RectiCare, LMX5, Dr. Numb)
anorectal gel
- 5% (Topicaine 5)
Hemorrhoids or Anorectal Pain
Indicated for pain, itching, and burning associated with hemorrhoids and other anorectal disorders
<12 years: Safety and efficacy not established
≥12 years: Apply to perianal region up to 6 times/day
Not to be used inside the rectum
Administration
Not to be used inside the rectum
When practical, clean area with soap and water, and gently pat dry before use
Adverse Effects
Frequency Not Defined
Application site reactions
- Abnormal sensation
- Pallor or blanching when the application time is very prolonged (>2 hr)
- Alterations in temperature sensations
- Edema
- Itching
- Rash
Systemic reactions
- Unlikely due to the small dose absorbed; may occur with repeated doses or application to large surface area (see Cautions)
- CNS excitation and/or depression
- Light-headedness, nervousness, apprehension, euphoria, confusion
- Dizziness
- Drowsiness
- Tinnitus
- Blurred or double vision
- Vomiting
- Sensations of heat, cold or numbness
- Twitching, tremors, convulsions
- Unconsciousness, respiratory depression, and arrest
- Cardiovascular manifestations (eg, bradycardia, hypotension, and cardiovascular collapse leading to arrest)
Warnings
Contraindications
Hypersensitivity to amide-type anesthetics
Cautions
Do not apply to eyes, ears, or mucous membranes
Severe hepatic impairment
Do not exceed recommended dosage unless directed by a doctor
Do not put this product into the rectum by using fingers or any mechanical device or applicator
Discontinue if
- Rectal bleeding occurs
- Condition worsens or does not improve within 7 days
- Allergic reaction occurs
- Symptom being treated does not subside or if redness, irritation, swelling, pain or other symptoms develop or increase
- Symptoms clear up and return within a few days
Extensive systemic absorption
- Can result in plasma levels that could, in susceptible individuals, produce a systemic pharmacologic response (also see Adverse Effects)
- Increased absorption may occur with:
- -Application to broken or inflamed skin
- -Application to ≥2,000 cm² of skin of an adult
- -Application to ≥600 cm² in children 10-20 kg body weight or ≥100 cm² in children up to 10 kg
Pregnancy & Lactation
Pregnancy
Ask healthcare professional before use
Lactation
Ask healthcare professional before use
Pregnancy Categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk. C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk. X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist. NA: Information not available.Pharmacology
Mechanism of Action
Amide-type local anesthetic; reversibly block the initiation and conduction of nerve impulses by interfering with the flux of sodium ions though the neuronal membrane
Pharmacokinetics
Onset, depth, and duration of dermal analgesia depend primarily on the site of application and duration of application
Onset of action: ~1 hr following application, and the effect persists for approximately 1 hr after removal; 30 minutes for areas such as the upper lip
