Navigation

lidocaine rectal (RectiCare, LMX5, Topicaine 5, Dr. Numb, H-Releve Hemorrhoidal)

 

Classes: Local Anesthetics, Amides; Anesthetics, Topical

Dosing and uses of RectiCare, LMX 5 (lidocaine rectal)

 

Adult dosage forms and 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

 

Pediatric dosage forms and 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

 

RectiCare, LMX 5 (lidocaine rectal) adverse (side) 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

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 and lactation

Pregnancy category: B

Lactation: Distributed in human breast milk with extensive systemic absorption; milk:plasma ratio = 0.4

Pregnant or breastfeeding patients should seek advice of health professional before using OTC drugs

 

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 of RectiCare, LMX 5 (lidocaine rectal)

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