Oxybutynin (Ditropan) is an anticholinergic (antimuscarinic) drug that is used to treat overactive bladder manifesting s urinary urgency, frequency, and incontinence.

Oxybutynin Uses:

Overactive bladder:

• Used for treatment of symptoms associated with overactive bladder (eg, urge urinary incontinence, urgency, frequency, urinary leakage, dysuria).
• Used for treatment of symptoms associated with overactive bladder due to a neurological condition (eg, spina bifida) in patients ≥6 years of age (extended-release tablet only).

Off Label Use of Oxybutynin in Adults:

• Primary focal hyperhidrosis

Oxybutynin Dose in Adults

Oxybutynin Dose in the treatment of Overactive bladder (urinary urgency with or without incontinence):

Note:

• Consider use after inadequate response to or in conjunction with nonpharmacologic measures.
• The full benefit may not be observed until after several weeks of treatment.
• A trial of ≥4 to 12 weeks, including the titration period if needed to optimize dose, is suggested before considering other options.
• Antimuscarinic agents are not recommended in patients with stress type incontinence.

Extended-release oral tablets:

Note: Extended-release formulations are preferred due to improved tolerability.

• Initial: 5 to 10 mg orally once a day.
• Adjust dose as needed and tolerated in 5 mg increments every 1 to ≥2 weeks.
• Maximum: 30 mg once a day.

Immediate-release oral tablets:

• 5 mg 2 to 3 times daily.
• Adjust dose as needed and tolerated in 5 mg increments every 1 to ≥2 weeks.
• In patients with overactive bladder associated with neurodegenerative diseases, may consider initiation at 2.5 mg 2 to 3 times daily.
• Maximum: 5 mg 4 times daily.

Note:

• In patients with nocturia, some experts suggest a single daily dose of 2.5 to 5 mg at bedtime may be sufficient.

Topical gel:

• Apply contents of 1 sachet (100 mg/g) or 1 actuation of the pump (100 mg/g) once daily.

Transdermal:

• Apply one 3.9 mg/day patch twice weekly (every 3 to 4 days); change the patch on the same 2 days each week.

OTC labeling (patient-guided therapy):

• Females: Apply one 3.9 mg/day patch every 4 days.

Oxybutynin Dose in the treatment of primary focal hyperhidrosis as an alternative agent (off-label): Oral:

Extended-release:

• 5 to 10 mg once a day.

Immediate release:

• Initial: 2.5 mg once a day.
• Gradually titrate as needed and tolerated.
• Usual effective dose range: 5 to 10 mg per day in 2 divided doses.

Oxybutynin Dose in Childrens

Oxybutynin Dose in the treatment of Neurogenic and Overactive bladder:

Immediate release:

Infants and Children ≤5 years:

• Limited data available:

  • 0.1 to 0.2 mg/kg/dose 2 to 3 times daily;
  • maximum dose: 5 mg/dose
  • one retrospective study reported doses as high 0.2 mg/kg/dose every 6 hours.

• Children >5 years and Adolescents:

  • Initial: 5 mg twice a day, increase as necessary up to 5 mg 3 times daily;
  • adult maximum dose: 5 mg 4 times daily

Extended-release:

Children ≥6 years and Adolescents:

• 5 mg once a day initially.
• Adjust dose as needed in 5 mg increments at weekly intervals.
• Maximum daily dose: 20 mg per day.

Oxybutynin Intravesical Dose: Limited data available:

Infants, Children, and Adolescents:

• 2 mg/kg/dose twice a day at 8 to 12-hour intervals.
• Maximum dose: 5 mg/dose.

Oxybutynin dose in the treatment of Idiopathic Overactive bladder: Transdermal:

Children ≥4 years and Adolescents:

• Apply one 3.9 mg per day patch twice weekly (every 3 to 4 days).
• Dosing based on a retrospective study of 35 children (mean age: 8 years; range: 4 to 16 years) with idiopathic overactive bladder.
• Most patients (97%) reported good symptom control.
• Skin irritation at the application site was reported in 35% of patients with 20% resulting in discontinuation of therapy.
• No other significant side effects were reported.

Pregnancy Risk Factor B

• Animal reproduction studies did not show any adverse events.
• Limited information is available on the use of oxybutynin during pregnancy in patients with neurogenic bladder.

Oxybutynin use during breastfeeding:

• It is unknown if breast milk contains oxybutynin.
• According to the manufacturer breastfeeding during therapy is a decision that should be made after considering the risks to infants and the benefits to mothers.
• Reports have indicated that lactation suppression has been occurring.

Oxybutynin Dose in Kidney Disease:

• In the manufacturer's labeling there are no dosage adjustments provided  (has not been studied).
• Use cautiously.

Oxybutynin Dose in Liver Disease:

• In the manufacturer's labeling there are no dosage adjustments provided  (has not been studied)
• Use cautiously.

Common Side Effects of Oxybutynin:

• Central Nervous System:

  • Dizziness
  • Drowsiness

• Gastrointestinal:

  • Xerostomia
  • Constipation
  • Nausea

• Local:

  • Application Site Pruritus

Less Common Side Effects Of Oxybutynin:

• Cardiovascular:

  • Decreased Blood Pressure
  • Edema
  • Flushing
  • Increased Blood Pressure
  • Palpitations
  • Peripheral Edema
  • Sinus Arrhythmia

• Central Nervous System:

  • Headache
  • Nervousness
  • Insomnia
  • Confusion
  • Falling
  • Flank Pain
  • Pain
  • Fatigue

• Dermatologic:

  • Macular Eruption
  • Xeroderma
  • Pruritus

• Endocrine & Metabolic:

  • Fluid Retention
  • Increased Thirst
  • Increased Serum Glucose

• Gastrointestinal:

  • Diarrhea
  • Dyspepsia
  • Coated Tongue
  • Eructation
  • Upper Abdominal Pain
  • Flatulence
  • Abdominal Pain
  • Dysgeusia
  • Viral Gastroenteritis
  • Vomiting
  • Gastroesophageal Reflux Disease

• Genitourinary:

  • Urinary Hesitancy
  • Urinary Tract Infection
  • Urinary Retention
  • Cystitis
  • Pollakiuria
  • Increased Postvoid Residual Urine Volume
  • Dysuria

• Infection:

  • Fungal Infection

• Local:

  • Application Site Erythema
  • Application Site Reaction
  • Application Site Rash
  • Application Site Vesicles
  • Application Site Dermatitis

• Neuromuscular & Skeletal:

  • Arthralgia
  • Back Pain
  • Limb Pain
  • Asthenia

• Ophthalmic:

  • Blurred Vision
  • Eye Irritation
  • Keratoconjunctivitis Sicca
  • Visual Disturbance
  • Xerophthalmia

• Respiratory:

  • Dry Nose
  • Upper Respiratory Tract Infection
  • Asthma
  • Bronchitis
  • Hoarseness
  • Nasal Congestion
  • Nasopharyngitis
  • Paranasal Sinus Congestion
  • Pharyngolaryngeal Pain
  • Sinus Headache
  • Cough
  • Dry Throat
  • Oropharyngeal Pain

Contraindications to Oxybutynin:

• Hypersensitivity to oxybutynin and any other component of the formulation
• Patients who have uncontrolled narrow-angle or high-risk glaucoma
• Urinary retention
• Conditions with severe GI motility or gastric retention.

OTC labeling

• Self-medication should not be used if there is pain or burning in the urit, blood in the urine, side or lower back pain, or a cloudy or foul-smelling bladder.
• For males, age 18 Years
• Only cough, sneeze, or laugh can cause accidental urine loss;
• Diagnosis of gastric or urinary retention
• glaucoma;
• Hypersensitivity to Oxybutynin

Canadian labeling:Additional contraindications not listed in the US labeling:

• Grave GI conditions.
• myasthenia gravis.

Warnings and precautions

• Hypersensitivity reactions and angioedema:

  • Hypersensitivity may include anaphylaxis or angioedema.
  • Oral oxybutynin has been used to treat angioedema of the lips, face, tongue, larynx, and/or tongue. Some cases were reported after only one dose.
  • If you have a problem with your tongue, hypopharynx or larynx, stop immediately
  • You must immediately take the appropriate management steps.

• CNS effects

  • Anticholinergics can cause confusion, agitation, drowsiness and dizziness as well as headaches, blurred vision, hallucinations, hallucinations, hallucinations, hallucinations, hallucinations, hallucinations, hallucinations, headaches, somnolence and/or blurred sight. These effects may lead to impairment of mental or physical abilities.
  • It is important to warn patients about tasks that require mental alertness, such as driving or operating machinery.
  • Dose reduction or discontinuation is recommended if there are any CNS side effects.

• Heat prostration:

  • Increased risk of heat prostration

• Bladder flow obstruction

  • Patients with obstruction of bladder flow should be cautious
  • This may increase the likelihood of urinary retention.

• Cardiovascular disease

  • Patients with CAD, heart disease, hypertension and/or cardiac arrhythmias should be treated with caution
  • This could make the condition worse.

• Dementia

  • Patients with dementia who have been treated with cholinesterase inhibitors should be cautious.
  • This may lead to more severe symptoms.

• GI disorders

  • Patients with GI obstructive or decreased GI motility should be cautious.
  • Increased risk of gastric retention
  • Patients with ulcerative colitis or intestinal atony, pyloric reflux, or medications that can cause or exacerbate esophagitis (eg bisphosphonates) should be cautious.
  • Patients with ulcerative colitis may experience decreased gastric motility, which can increase the risk of toxic megacolon or paralytic ileus.

• Glaucoma:

  • Patients with angle-closure glaucoma should be treated cautiously
  • This could make the condition worse.
  • Uncontrolled narrow-angle vision impairment is a contraindication.

• Hepatic impairment

  • Be careful.

• Hiatal hernia

  • Be careful.

• Hyperthyroidism:

  • Be careful, as it may worsen the condition.

• Myasthenia gravis:

  • Patients with myasthenia gravis should be avoided.
  • This could make the condition worse.
  • If you experience any symptoms or signs, discontinue treatment.

• Neuropathy:

  • Be careful.

• Parkinson disease

  • Be careful.

• Prostatic hyperplasia, urinary stricture

  • It can cause urinary retention so be careful.

• Renal impairment

  • Be careful.

Monitoring Parameters:

• Incontinence episodes
• Postvoid residual (PVR)
• Anticholinergic reactions (eg, dry mouth, constipation, dizziness).

How to administer Oxybutynin?

Oral: Extended-release tablets:

• Administer without regard to meals.
• Must be swallowed whole with liquid.
• Do not crush, divide, or chew.
• Take at approximately the same time each day.

Topical gel:

• For topical use only.
• Apply to clean, dry, intact skin on the abdomen, thighs, or upper arms/shoulders.
• Rotate application sites.
• Do not apply to the same site on consecutive days.
• Wash hands after use.
• Cover treated area with clothing after the gel has dried to prevent transfer of medication to others.
• Do not bathe, shower, or swim until 1 hour after gel applied.
• Do not apply to recently shaved skin.

Pump:

• Prior to initial use, prime pump several times (≥ 4 times) until gel begins to come out.
• After gel is observed, fully depress the pump one more time and discard gel dispensed from pump during priming.
• One full depression of the pump provides one dose.
• Discard after 30 doses.

Transdermal:

• Apply to clean, dry, smooth (fold-free) skin on the abdomen, hip, or buttock.
• Do not apply to areas treated with oils, lotions, or powders.
• Do not apply to areas with cuts, scrapes, or other irritation (ie, rashes).
• Do not cut the patch.
• Apply each system at a new site (avoid reapplication to the same site within 7 days).
• Contact with water while bathing, swimming, showering, or exercising will not change the effect.
• However, rubbing of the patch area should be avoided during these activities.
• The patch should be worn under clothing.
• Do not expose to sunlight.

Mechanism of action of Oxybutynin:

• Direct antispasmodic effect on smooth muscle, also inhibits the action of acetylcholine on smooth muscle (exhibits / the anticholinergic activity of atropine, but has 4-10 times the antispasmodic activity).
• It doesn't block the effects of skeletal muscle and autonomic ganglia.
• It increases bladder capacity, decreases uninhibited contractions, and delays the desire to void. This decreases urgency and frequency.

The onset of action:

• Oral: Immediate release: 30 to 60 minutes.

Peak effect:

• Immediate-release: 3 to 6 hours;
• Extended-release: 3 days

Duration:

• Oral: Immediate release: 6 to 10 hours;
• Extended-release: Up to 24 hours;
• Transdermal 96 hours

Absorption:

• Oral: Rapid and well absorbed;
• Transdermal: High

Protein binding:

• >99% primarily to alpha-1 acid glycoprotein

Metabolism:

• Hepatic via CYP3A4; Oral:
• High first-pass metabolism; forms active and inactive metabolites

Bioavailability:

• Oral: Immediate release: 6% (range: 1.6% to 10.9%)

Half-life elimination:

• IV: ~2 hours (parent drug), 7 to 8 hours (metabolites).
• Oral: Immediate release: ~2 to 3 hours;
• Extended-release: ~13 hours;
• Transdermal: 64 hours

Time to peak serum concentration:

• Oral: Immediate release: ~60 minutes;
• Extended-release: 4 to 6 hours;
• Transdermal: 24 to 48 hours

Excretion:

• Urine (<0.1% as metabolites and unchanged drug)

International Brands of Oxybutynin:

• Ditropan XL
• Gelnique
• Gelnique Pump
• Oxytrol
• Oxytrol For Women
• APO-Oxybutynin
• Ditropan XL
• DOM-Oxybutynin
• Gelnique
• MYLAN-Oxybutynin
• Oxytrol
• PHLOxybutynin
• PMS-Oxybutynin
• RIVA-Oxybutynin
• TEVA-Oxybutynin
• Ao Ning
• Butyn
• Contimax
• Cystrin
• Delifon
• Detronin
• Ditropan
• Ditropan XL
• Diutropan
• Dresplan
• Dridase
• Driptane
• Frenurin
• Gradual
• Inprax
• Kentera
• Kentera Patch
• Lenditro
• Lyrinel
• Lyrinel Oros SR
• Lyrinel XL
• Mutum
• Mutum CR
• Nefryl
• Neoxy Tape
• Newin
• Novitropan
• Obutin
• Odranal
• Oxurate
• Oxyban
• Oxyspas
• Oxytrol
• Pollakisu
• Reteven
• Sibutin
• Socliden
• Tavor
• Tropan
• Uricon CR
• Urihexal
• Uroflax
• Uropan
• Uroxal

Oxybutynin Brand Names in Pakistan:

Oxybutynin 3 mg Tablets
Butyn	Figs Pharmaceuticals
Oxitrin	Dr. Raza Pharma (Private) Limited
Oxynin	Venus Pharma
Taivor	Raazee Theraputics (Pvt) Ltd.

Oxybutynin 5 mg Tablets
Cystrin	A.J. & Company.
Oxitrin	Dr. Raza Pharma (Private) Limited
Oxityn	Rakaposhi Pharmaceutical (Pvt) Ltd.
Oxycystin	Pulse Pharmaceuticals
Oxynin-5	Venus Pharma