Hyoscyamine (Levsin) acts on the smooth muscles, secretory glands, and the central nervous system. It is used in the treatment of intestinal spasm, irritable bowel syndrome, anticholinesterase poisoning, and preoperatively as an antimuscarinic agent.

Hyoscyamine Uses:

• Anesthesia:

  • Preoperative antimuscarinic:
    • Preoperative antimuscarinic to reduce secretions like salivary, tracheobronchial, pharyngeal, and gastric secretions; to block cardiac vagal inhibitory reflexes during induction of anesthesia and intubation
  • Reversal of neuromuscular blockade and associated muscarinic effects:
    • Protects against peripheral muscarinic effects (such as bradycardia and excessive secretions produced by halogenated hydrocarbons and cholinergic agents [such as physostigmine, neostigmine, and pyridostigmine]) given to reverse actions of curariform agents

• An antidote for anticholinesterase agent poisoning:

  • It is an antidote in anticholinesterase agent poisoning.

• Biliary and renal colic:

  • It can be used for symptomatic treatment of renal and biliary colic as adjunctive therapy along with morphine or other opioid agents.

• Diagnostic procedures:

  • It decreases the gastrointestinal motility and aids diagnostic procedures i.endoscopy or hypotonic duodenography.

• GI disorders:

  • Help in controlling acute episodes of gastric secretion, visceral spasm, hypermotility in spastic colitis, pylorospasm, and associated abdominal cramps; relieve symptoms in functional intestinal disorders (eg, mild dysenteries, diverticulitis) and infant colic (elixir and oral solution)
  • Adjunctive therapy for treatment in peptic ulcer; irritable bowel syndrome (irritable colon, spastic colon, acute enterocolitis, mucous colitis) and other functional GI disorders; neurogenic bowel disturbances (including splenic flexure syndrome and neurogenic colon)

• Pancreatitis:

  In pancreatitis may relieve pain and reduces secretion.

• Parkinsonism:

  • Reduce rigidity and tremors and to control associated sialorrhea and hyperhidrosis in parkinsonism.

• Partial heart block:

  • For use in certain cases of partial heart block associated with vagal activity

• Rhinitis:

  • Effective in acute rhinitis as a drying agent.

• Urinary system disorder:

  • To control hypermotility in spastic bladder and cystitis; adjunctive therapy in the treatment of neurogenic bladder

Hyoscyamine (Levsin) Dose in Adults

Hyoscyamine (Levsin) Dose in the treatment of Gastrointestinal disorders:

Oral:

• Tablet, dispersible:

  • Anaspaz, ED-SPAZ, NuLev:
    • 0.125 to 0.25 mg every 4 hours or as needed;
    • maximum: 1.5 mg/day
  • Oscimin:
    • 0.125 to 0.25 mg 3 to 4 times daily;
    • may increase to every 4 hours as needed;
    • maximum: 1.5 mg/day

• Tablet, extended-release:

  • Levbid:
    • 0.375 to 0.75 mg every 12 hours;
    • maximum: 1.5 mg/day
  • Oscimin SR, Symax Duotab, Symax SR:
    • 0.375 to 0.75 mg every 12 hours or 0.375 mg every 8 hours;
    • maximum: 1.5 mg/day

• Tablet, regular release:

  • Levsin:
    • 0.125 to 0.25 mg every 4 hours or as needed;
    • maximum: 1.5 mg/day
  • Oscimin:
    • 0.125 to 0.25 mg 3 to 4 times daily;
    • may increase to every 4 hours as needed;
    • maximum: 1.5 mg/day
• Tablet, sublingual (Levsin/SL, Oscimin, Symax SL):
  • 0.125 to 0.25 mg 3 to 4 times daily;
  • may increase to every 4 hours as needed; maximum: 1.5 mg/day

Drops (Hyosyne [0.125 mg/mL]):

• 0.125 mg (1 mL) to 0.25 mg (2 mL) every 4 hours or as needed;
• The maximum: 1.5 mg (12 mL) per day
• Elixir (Hyosyne [0.125 mg/5 mL]):
  • 0.125 mg (5 mL) to 0.25 mg (10 mL) every 4 hours or as needed;
  • maximum: 1.5 mg (60 mL) per day

IM, IV, SubQ:

• 0.25 to 0.5 mg;
• may repeat as needed up to 4 times daily, at 4-hour intervals

Hyoscyamine (Levsin) Dose in the Diagnostic procedures:

• Intravenous: 0.25 to 0.5 mg given 5 to 10 minutes before  procedure

Hyoscyamine (Levsin) Dose in the Preanesthesia:

• Intramascular, Intravenous, SubQ:
  • 5 mcg/kg given 30 to 60 minutes before induction of anesthesia or at the time of administration of preoperative opioids or sedatives.

Hyoscyamine (Levsin) Dose to reduce drug-induced bradycardia during surgery:

• Intravenous: 0.125 mg; repeat as needed

Hyoscyamine (Levsin) Dose for the reversal of neuromuscular blockade:

• IM, IV, SubQ:
  • 0.2 mg for every 1 mg neostigmine (or the physostigmine/pyridostigmine equivalent)

Hyoscyamine (Levsin) Dose in Childrens

Note:

• Oral dosage forms (drops and elixirs) are different (ie, 0.125 mg/mL [drops] and 0.125 mg/5 mL [solution]);
• Precaution should be taken to verify and avoid confusion between the different concentrations;
• The dose should be clearly presented with the corresponding product formulation.

Hyoscyamine (Levsin) Dose in the treatment of Gastrointestinal and urinary systemic spasms (including infant colic, biliary and renal colic):

• Infants and Children <2 years: Oral: Drops (eg, Hyosyne [0.125 mg/mL]):
• Do not exceed 6 doses in 24 hours
  • 4 to <5 kg:
    • 0.01375 mg (0.11 mL or 4 drops) every 4 hours or as needed;
    • The maximum daily dose: 0.0825 mg (0.66 mL or 24 drops)/day
  • 5 to <7 kg:
    • 0.0175 mg (0.14 mL or 5 drops) every 4 hours or as needed;
    • The maximum daily dose: 0.105 mg (0.84 mL or 30 drops)/day
  • 7 to <10 kg:
    • 0.02 mg (0.16 mL or 6 drops) every 4 hours or as needed;
    • The maximum daily dose: 0.12 mg (0.96 mL or 36 drops)/day
  • ≥10 kg:
    • 0.0275 mg (0.22 mL or 8 drops) every 4 hours or as needed;
    • The maximum daily dose: 0.165 mg (1.32 mL or 48 drops)/day

• Children 2 to <12 years: Oral:

  • Drops (eg, Hyosyne [0.125 mg/mL]):
    • 0.03125 mg (0.25 mL) to 0.125 mg (1 mL) every 4 hours or as needed;
    • The maximum daily dose: 0.75 mg (6 mL)/day;
    • Do not exceed 6 doses in 24 hours

  • Elixir (eg, Hyosyne [0.125 mg/5 mL]): Do not exceed 6 doses in 24 hours:

    • 10 to <20 kg:
      • • 0.03125 mg (1.25 mL) every 4 hours or as needed;
        • The maximum daily dose: 0.1875 mg (7.5 mL)/day
    • 20 to <40 kg:
      • • 0.0625 mg (2.5 mL) every 4 hours or as needed;
        • maximum daily dose: 0.375 mg (15 mL)/day
    • 40 to <50 kg:
      • • 0.09375 mg (3.75 mL) every 4 hours or as needed;
        • The maximum daily dose: 0.5625 mg (22.5 mL)/day
    • ≥50 kg:
      • 0.125 mg (5 mL) every 4 hours or as needed;
      • maximum daily dose: 0.75 mg (30 mL)/day

    • Tablets, immediate-release:

      • Regular tablet [Levsin], sublingual [Levsin/SL], dispersible [Anaspaz, ED-SPAZ, NuLev]):
        • 0.0625 to 0.125 mg every 4 hours or as needed;
        • The maximum daily dose: 0.75 mg/day

• Children ≥12 years and Adolescents: Oral:

  • Immediate-release:

    • Drops (Hyosyne [0.125 mg/mL]):
      • 0.125 mg (1 mL) to 0.25 mg (2 mL) every 4 hours or as needed;
      • The maximum daily dose: 1.5 mg (12 mL)/day
    • Elixir (Hyosyne [0.125 mg/5 mL]):
      • 0.125 mg (5 mL) to 0.25 mg (10 mL) every 4 hours or as needed;
      • maximum daily dose: 1.5 mg (60 mL)/day

    • Tablet, Dispersible:

      • Anaspaz, ED-SPAZ, NuLev:
        • 0.125 to 0.25 mg every 4 hours or as needed;
        • maximum daily dose: 1.5 mg/day
      • Oscimin:
        • 0.125 to 0.25 mg 3 to 4 times daily;
        • may increase to every 4 hours as needed;
        • maximum daily dose: 1.5 mg/day

    • Tablets:

      • Levsin:
        • 0.125 to 0.25 mg every 4 hours or as needed;
        • maximum daily dose: 1.5 mg/day
      • Oscimin:
        • 0.125 to 0.25 mg 3 to 4 times daily;
        • may increase to every 4 hours as needed;
        • maximum daily dose: 1.5 mg/day

    • Sublingual Tablets:

      • Levsin/SL:
        • 0.125 to 0.25 mg every 4 hours or as needed;
        • maximum daily dose: 1.5 mg/day
      • Oscimin, Symax SL:
        • 0.125 to 0.25 mg 3 to 4 times daily;
        • may increase to every 4 hours as needed;
        • maximum daily dose: 1.5 mg/day

  • Extended release: Tablet:

    • Levbid:
      • 0.375 to 0.75 mg every 12 hours;
      • maximum daily dose: 1.5 mg/day
    • Oscimin SR, Symax Duotab, Symax SR:
      • 0.375 to 0.75 mg every 12 hours OR
      • 0.375 mg every 8 hours;
      • Maximum daily dose: 1.5 mg/day

Hyoscyamine (Levsin) Dose in the Preanesthesia:

• Children >2 years and Adolescents:

  • IM, IV, SubQ:
    • 5 mcg/kg administered half an hour before induction of anesthesia or at the time of administrating preoperative opioids or sedatives.

Hyoscyamine (Levsin) Dose in the Reduce drug-induced bradycardia during surgery:

• Children >2 years and Adolescents:

  • IV: 0.125 mg;
  • repeat as needed

Hyoscyamine (Levsin) Dose in the Reversal of neuromuscular blockage:

• Children >2 years and Adolescents:

  • IV, IM, SubQ:
    • 0.2 mg for every 1 mg neostigmine (or physostigmine/ pyridostigmine equivalent)

Pregnancy Risk Factor C

• Hyoscyamine crosses the placental barrier

Hyoscyamine use during breastfeeding:

• Breast milk contains trace amounts of hyoscyamine.
• Nursing mothers should exercise caution.

Dose in Kidney Disease:

No dosage adjustment is provided by manufacturers, use with cautions.

Dose in Liver disease:

There are no dosage adjustments provided in the manufacturer’s labeling, use with caution.

Side effects of Hyoscyamine (Levsin):

• Cardiovascular:

  • Flushing
  • Palpitations
  • Tachycardia

• Central Nervous System:

  • Amnesia
  • Ataxia
  • Confusion
  • Dizziness
  • Drowsiness
  • Excitement
  • Fatigue
  • Hallucination
  • Headache
  • Insomnia
  • Nervousness
  • Psychosis
  • Speech Disturbance

• Dermatologic:

  • Hypohidrosis
  • Urticaria

• Gastrointestinal:

  • Abdominal Pain
  • Ageusia
  • Bloating
  • Constipation
  • Diarrhea
  • Dysgeusia
  • Dysphagia
  • Heartburn
  • Nausea
  • Vomiting
  • Xerostomia

• Genitourinary:

  • Decreased Lactation
  • Impotence
  • Urinary Hesitancy
  • Urinary Retention

• Hypersensitivity:

  • Hypersensitivity Reaction

• Neuromuscular & Skeletal:

  • Weakness

• Ophthalmic:

  • Blurred Vision
  • Cycloplegia
  • Increased Intraocular Pressure
  • Mydriasis

• Miscellaneous:

  • Fever

Contraindications to Hyoscyamine (Levsin):

• Hypersensitivity to the belladonna alkaloids and any component of this formulation
• glaucoma;
• Obstructive uropathy (eg bladder neck obstruction caused by prostatic hypertrophy);
• myasthenia gravis;
• obstructive GI tract diseases (eg, achalasia), pyloroduodenal stenosis, paralytic ileus; severe ulcerative colitis. Toxic megacolon complicating ulcerative bowel colitis.
• Instable cardiovascular condition
• myocardial ischemia.

Notification

• Extended-release products may not be recommended for children under 12 years old. Refer to the labeling.

Warnings and precautions

• CNS effects

  • It may be harmful to mental activities and may cause blurred vision or drowsiness.

• Diarrhea:

  • This could be incomplete intestinal obstruction in patients with ileostomy and colostomy. If this happens, it should be stopped immediately.

• Heat prostration:

  • In hot climates, heat prostration can occur. Exercise caution and be careful in hot weather

• Oral effects

  • Long-term use can cause gum disease, periodontal disease, and discomfort from decreased salivation.

• Psychosis:

  • Patients with extreme anticholinergic effects sensitivity may experience psychosis. It usually resolves in 12-48 hours.

• Cardiovascular disease

  • Patients with heart disease (e.g. coronary artery disease), tachyarrhythmias or heart failure) should be cautious.
  • Before initiating drug therapy, it is important to evaluate for tachycardia. Suspected heart disease patients should not use it.

• Hiatal hernia

  • Patients with reflux esophagitis should be cautious.

• Hyperthyroidism:

  • Patients with thyrotoxicosis should be cautious.

• Neuropathy:

  • Patients with autonomic nervepathy should be cautious.

• Prostatic hyperplasia

  • Patients with prostatic hyperplasia should be cautious.

• Renal impairment

  • Patients with impaired renal function should be cautious.

Hyoscyamine: Drug Interaction

Monitoring Parameters:

None mentioned.

How to administer Hyoscyamine?

Oral:

• Elixir (Hyosyne):
  • Administration prior to meals (~30 to 60 minutes) is recommended (but not required) when used to treat gastrointestinal disorders.
• Drops (Hyosyne):
  • Administration prior to meals (~30 to 60 minutes) is recommended (but not required) when used to treat gastrointestinal disorders.
  • Use the provided dropper to accurately measure the dose.
• Tablet, regular release (Levsin, Oscimin):
  • Administration prior to meals (~30 to 60 minutes) is recommended (but not required) when used to treat gastrointestinal disorders.
• Tablet, dispersible:
  • Administration prior to meals (~30 to 60 minutes) is recommended (but not required) when used to treat gastrointestinal disorders.
• Anaspaz:
  • Tablets may be used sublingually, chewed, or swallowed whole.
• Ed-Spaz:
  • Place on top of the tongue and allow to dissolve;
  • Swallow with saliva.
• NuLev, Oscimin:
  • Tablets may be chewed or placed on the tongue and allowed to disintegrate.
• Tablet, extended-release:
  • Administration prior to meals (~30 to 60 minutes) is recommended (but not required) when used to treat gastrointestinal disorders.
• Levbid:
  • Do not crush or chew.
• Oscimin SR, Symax Duotab, Symax SR:
  • Swallow whole.
• Tablet, sublingual:
  • The recommended way is to take the drug 30 - 60 minutes before a meal, (but not required) when used to treat gastrointestinal disorders.
• Levsin/SL:
  • Tablets may be used sublingually, chewed, or swallowed whole.
• Symax SL:
  • use tablets sublingually or swallowed whole.
• Oscimin:
•  sublingual administration.

IM:

• Without dilution can inject intramuscularly.

IV:

• Inject over at least 1 minute without dilution.

SubQ:

• can inject without dilution

Mechanism of action of Hyoscyamine:

It prevents acetylcholine from acting at parasympathetic locations in smooth muscle, secretory and central nervous systems. It increases cardiac output and dries secretions.

The beginning of action:

• 2 to 3 minutes

Duration:

• Regular release: 4 to 6 hours;
• Extended-release (Levbid, Symax Duotab): 8 to 12 hours

Absorption:

• Well absorbed

Metabolism:

• Hepatic

Half-life elimination:

• Regular release: 2 to 3.5 hours;
• Extended-release (Levbid): ~7 hours

Excretion:

• Urine

International Brand Names of Hyoscyamine:

• Anaspaz
• Ed-Spaz
• Hyosyne
• Levbid
• Levsin
• Levsin/SL
• NuLev
• Oscimin
• Oscimin SR
• Symax Duotab
• Symax-SL
• Symax-SR
• Buwecon
• Duboisine
• Egacene
• Egazil Duretter
• Eyosin
• Levsin SL
• Neo-Allospasmin
• Nuspas

Hyoscyamine Brand Names in Pakistan: