Hyoscyamine is a natural alkaloid found in certain plants, particularly in the Solanaceae family, which includes plants like belladonna (Atropa belladonna), henbane (Hyoscyamus niger), and jimsonweed (Datura stramonium). These plants have a long history of medicinal use, as well as being known for their toxic properties.

Hyoscyamine belongs to a class of compounds known as tropane alkaloids. It has antimuscarinic properties, meaning it blocks the action of acetylcholine, a neurotransmitter, at muscarinic receptors. This results in various physiological effects, including smooth muscle relaxation and decreased glandular secretions.

Hyoscyamine (Levsin) acts on the smooth muscles, secretory glands, and the central nervous system. It is used in the treatment of intestinal spasms, 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 for 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.
• GI disorders:
  • Adjunctive therapy is used to treat peptic ulcers, irritable bowel syndrome, acute enterocolitis, mucous colitis, and other functional GI diseases, as well as neurogenic bowel disturbances (including splenic flexure syndrome and neurogenic colon)
  • Controlling acute bouts of gastric secretion, visceral spasm, hypermotility in spastic colitis, pylorospasm, and related stomach pains; reducing the symptoms of functional intestinal illnesses (such as mild dysentery and diverticulitis), as well as newborn colic (elixir and oral solution)
• Diagnostic procedures:
  • It decreases gastrointestinal motility and aids diagnostic procedures i.endoscopy or hypotonic biodemography.
• Pancreatitis:

Pain and secretion may be reduced by pancreatitis.

• Partial heart block:
  • To be used in specific instances of partial heart block brought on by vagal activity
• Parkinsonism:
  • Reduce tremors and stiffness, and manage sialorrhea and hyperhidrosis that are related to parkinsonism.
• Urinary system disorder:
  • Controlling bladder hypermotility in cases of cystitis and spastic bladder; adjuvant therapy for neurogenic bladder
• Rhinitis:
  • As a drying agent, it works well for acute rhinitis.

Hyoscyamine (Levsin) Dose in Adults

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

Oral Tablets (Dispersible):

• Anaspaz, ED-SPAZ, NuLev: 0.125 to 0.25 mg every 4 hours or as needed; don't take more than 1.5 mg/day.
• Oscimin: 0.125 to 0.25 mg 3 to 4 times daily; may increase to every 4 hours if needed; maximum: 1.5 mg/day.

Oral Tablets (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.

Oral Tablets (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 if needed; maximum: 1.5 mg/day.

Sublingual Tablets (Dissolve under the tongue):

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

Liquid Drops (Hyosyne [0.125 mg/mL]):

• Take 0.125 mg (1 mL) to 0.25 mg (2 mL) every 4 hours or as needed; maximum: 1.5 mg (12 mL) per day.

Liquid Elixir (Hyosyne [0.125 mg/5 mL]):

• Take 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.

Injection (IM, IV, SubQ):

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

Hyoscyamine (Levsin) Dose in the Pre anesthesia:

• The dose is 5 micrograms (mcg) per kilogram of body weight.
• It's given through an injection in the muscle (IM), intravenously (IV), or under the skin (SubQ).
• Administer it 30 to 60 minutes before the anesthesia is induced or when preoperative opioids or sedatives are given.

Hyoscyamine (Levsin) Dose in the Diagnostic procedures:

Intramuscular, Intravenous, SubQ:

• The dose is 0.25 to 0.5 mg.
• It's given 5 to 10 minutes before the procedure.

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

If you need to reverse the effects of certain medications that affect muscle function (neuromuscular blockade) using Hyoscyamine:

• The dose is 0.2 mg of Hyoscyamine for every 1 mg of neostigmine.
• This can be given through an injection in the muscle (IM), intravenously (IV), or under the skin (SubQ).

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

• The initial dose is 0.125 mg given through an IV.
• It can be repeated as needed, depending on the situation.

Hyoscyamine (Levsin) Dose in Children

Note:

• If you're taking Hyoscyamine in oral forms like drops or elixirs, be aware that there are different concentrations.
• For example, drops have 0.125 mg per milliliter (0.125 mg/mL), while elixirs have 0.125 mg in every 5 milliliters (0.125 mg/5 mL).
• To avoid confusion, always check and make sure you're using the right concentration.
• The prescribed dose should be clearly communicated along with the specific product formulation you're using.

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

Infants and Children under 2 years:

• Oral Drops (e.g., Hyosyne [0.125 mg/mL]):
  • 3.4 to <5 kg: 0.01375 mg (4 drops) every 4 hours; max daily: 0.0825 mg (24 drops)
  • 5 to <7 kg: 0.0175 mg (5 drops) every 4 hours; max daily: 0.105 mg (30 drops)
  • 7 to <10 kg: 0.02 mg (6 drops) every 4 hours; max daily: 0.12 mg (36 drops)
  • ≥10 kg: 0.0275 mg (8 drops) every 4 hours; max daily: 0.165 mg (48 drops)

Children 2 to <12 years:

• Oral Drops:
  • 0.03125 mg (0.25 mL) to 0.125 mg (1 mL) every 4 hours; max daily: 0.75 mg (6 mL)
• Oral Elixir (e.g., Hyosyne [0.125 mg/5 mL]):
  • 10 to <20 kg: 0.03125 mg (1.25 mL) every 4 hours; max daily: 0.1875 mg (7.5 mL)
  • 20 to <40 kg: 0.0625 mg (2.5 mL) every 4 hours; max daily: 0.375 mg (15 mL)
  • 40 to <50 kg: 0.09375 mg (3.75 mL) every 4 hours; max daily: 0.5625 mg (22.5 mL)
  • ≥50 kg: 0.125 mg (5 mL) every 4 hours; max daily: 0.75 mg (30 mL)
• Tablets (Immediate Release): 0.0625 to 0.125 mg every 4 hours; max daily: 0.75 mg/day

Children ≥12 years and Adolescents:

• Oral Drops (Hyosyne [0.125 mg/mL]):
  • 0.125 mg (1 mL) to 0.25 mg (2 mL) every 4 hours; max daily: 1.5 mg (12 mL)
• Oral Elixir (Hyosyne [0.125 mg/5 mL]):
  • 0.125 mg (5 mL) to 0.25 mg (10 mL) every 4 hours; max daily: 1.5 mg (60 mL)
• Dispersible Tablets (e.g., Anaspaz, ED-SPAZ, NuLev): 0.125 to 0.25 mg every 4 hours; max daily: 1.5 mg
• Immediate Release Tablets (e.g., Levsin, Oscimin): 0.125 to 0.25 mg every 4 hours; max daily: 1.5 mg
• Sublingual Tablets (e.g., Levsin/SL, Oscimin, Symax SL): 0.125 to 0.25 mg every 4 hours; max daily: 1.5 mg
• Extended-Release Tablets (e.g., Levbid, Oscimin SR, Symax Duotab, Symax SR):
  • 0.375 to 0.75 mg every 12 hours; max daily: 1.5 mg, or 0.375 mg every 8 hours; max daily: 1.5 mg

Hyoscyamine (Levsin) Dose in the Pre anesthesia:

For preanesthesia in children over 2 years and adolescents:

• The dose is 5 micrograms (mcg) per kilogram of body weight.
• It can be given through an injection in the muscle (IM), intravenously (IV), or under the skin (SubQ).
• Administer it 30 to 60 minutes before the anesthesia is induced or when preoperative opioids or sedatives are given.

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

For reducing drug-induced bradycardia during surgery in children over 2 years and adolescents using Hyoscyamine (Levsin):

• The initial dose is 0.125 mg.
• It is given through an intravenous (IV) injection.
• If necessary, the dose can be repeated.

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

For the reversal of neuromuscular blockage in children over 2 years and adolescents using Hyoscyamine:

• The dose is 0.2 mg of Hyoscyamine for every 1 mg of neostigmine (or equivalent of physostigmine/pyridostigmine).
• This can be administered through intravenous (IV), intramuscular (IM), or subcutaneous (SubQ) injection.

Pregnancy Risk Factor C

• We don't have information from studies about how hyoscyamine might affect animals during pregnancy.
• However, we do know that hyoscyamine can pass from the mother to the baby through the placenta.

Hyoscyamine use during breastfeeding:

• Hyoscyamine is found in small amounts in breast milk.
• If a breastfeeding woman needs to take hyoscyamine, it's suggested to be cautious.
• It's advisable to consult with a healthcare professional before using it during breastfeeding to weigh the potential benefits against any possible risks.

Dose in Kidney Disease:

• The manufacturer's labeling does not specify any adjustments in dosage for individuals with renal impairment (kidney problems).
• However, it recommends using hyoscyamine with caution in such cases.

Dose in Liver disease:

• The manufacturer's labeling does not specify any dosage adjustments for individuals with hepatic impairment (liver problems) when using hyoscyamine.
• However, it advises using the medication with caution in such cases.

Side effects of Hyoscyamine (Levsin):

• Hypersensitivity:
  • Hypersensitivity Reaction
• Cardiovascular:
  • Flushing
  • Tachycardia
  • Palpitations
• Dermatologic:
  • Hypohidrosis
  • Urticaria
• Central Nervous System:
  • Confusion
  • Dizziness
  • Amnesia
  • Ataxia
  • Drowsiness
  • Hallucination
  • Headache
  • Excitement
  • Fatigue
  • Psychosis
  • Speech Disturbance
  • Insomnia
  • Nervousness
• Gastrointestinal:
  • Bloating
  • Constipation
  • Abdominal Pain
  • Ageusia
  • Diarrhea
  • Heartburn
  • Nausea
  • Dysgeusia
  • Dysphagia
  • Vomiting
  • Xerostomia
• Neuromuscular & Skeletal:
  • Weakness
• Genitourinary:
  • Urinary Hesitancy
  • Urinary Retention
  • Decreased Lactation
  • Impotence
• Miscellaneous:
  • Fever
• Ophthalmic:
  • Blurred Vision
  • Mydriasis
  • Cycloplegia
  • Increased Intraocular Pressure

Contraindications to Hyoscyamine (Levsin):

Hyoscyamine should not be used in individuals with:

• Hypersensitivity to belladonna alkaloids or any component of the formulation.
• Glaucoma.
• Obstructive uropathy (such as bladder neck obstruction due to prostatic hypertrophy).
• Myasthenia gravis.
• Obstructive gastrointestinal tract disease (such as achalasia, pyloroduodenal stenosis).
• Paralytic ileus.
• Intestinal atony in elderly or debilitated patients.
• Severe ulcerative colitis.
• Toxic megacolon complicating ulcerative colitis.
• Unstable cardiovascular status.
• Myocardial ischemia.

Additionally, some extended-release products are not recommended in children under 12 years of age; it's advisable to refer to the manufacturer's labeling for specific guidance.

Notification

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

Warnings and precautions

CNS effects

• Hyoscyamine can have effects on the central nervous system (CNS), including causing drowsiness and/or blurred vision.
• These effects may impair physical or mental abilities.
• Patients taking hyoscyamine should be cautioned about engaging in activities that require mental alertness, such as operating machinery or driving.
• It's important for individuals to be aware of how hyoscyamine affects them personally and to avoid tasks that could be unsafe if they experience drowsiness or vision changes while taking the medication.

Diarrhea:

• If a person taking hyoscyamine experiences diarrhea, it could be a sign of incomplete intestinal obstruction, particularly in individuals with ileostomy or colostomy (surgical openings in the abdomen to redirect the flow of waste).
• In such cases, it's recommended to discontinue the treatment and seek medical attention.

Heat prostration:

• Hyoscyamine use carries the risk of heat prostration, especially in situations of elevated environmental temperatures.
• Caution is advised when using hyoscyamine in hot weather or during physical exercise.
• Heat prostration is a condition characterized by symptoms such as excessive heat, dehydration, and weakness.
• Individuals taking hyoscyamine should be mindful of their surroundings, stay hydrated, and avoid prolonged exposure to high temperatures, particularly when engaged in physical activities.
• If there are concerns or symptoms of heat-related issues, it's important to seek medical attention promptly.

Oral effects

Prolonged use of hyoscyamine may have effects on the mouth, including:

• Dental Caries: Increased risk of tooth decay.
• Periodontal Disease: Conditions affecting the gums and supporting structures of the teeth.
• Oral Candidiasis: Fungal infection in the mouth.
• Discomfort due to Decreased Salivation: Hyoscyamine can reduce saliva production, leading to discomfort in the mouth.

Individuals using hyoscyamine for an extended period should be aware of these potential oral effects. Maintaining good oral hygiene practices, such as regular dental check-ups and proper dental care, can help mitigate some of these risks.

Psychosis:

• In some cases, hyoscyamine can lead to a condition called psychosis, especially in individuals who are very sensitive to the medication's effects.
• Psychosis involves changes in thoughts, emotions, and perceptions that may not be in line with reality.
• Fortunately, this effect typically goes away on its own within 12 to 48 hours after stopping the medication.

Cardiovascular disease

• If you have cardiovascular disease, like coronary artery disease, tachyarrhythmias, heart failure, or hypertension, be cautious when using hyoscyamine.
• It's important to assess any rapid heart rate (tachycardia) before taking it.
• However, if you have unstable cardiovascular conditions or myocardial ischemia (inadequate blood flow to the heart muscle), using hyoscyamine is not recommended.

Hiatal hernia

• If you have a hiatal hernia with reflux esophagitis, use hyoscyamine with caution.
• Hiatal hernia is a condition where part of the stomach pushes into the chest through the diaphragm, and reflux esophagitis involves inflammation of the esophagus due to stomach acid flowing backward.
• Hyoscyamine use may require careful consideration in such cases.

Hyperthyroidism:

• If you have hyperthyroidism, use hyoscyamine with caution.
• Hyperthyroidism is a condition where the thyroid gland produces too much thyroid hormone.
• Hyoscyamine use may need careful monitoring in individuals with this condition.

Neuropathy:

• If you have autonomic neuropathy, use hyoscyamine with caution.
• Autonomic neuropathy affects the nerves that control involuntary bodily functions, including those of the digestive system.
• Hyoscyamine, by its anticholinergic effects, can influence these functions.

Prostatic hyperplasia

• If you have prostatic hyperplasia (enlargement of the prostate), use hyoscyamine with caution.
• This condition involves the enlargement of the prostate gland, which can cause urinary symptoms.
• Hyoscyamine may affect certain aspects of urinary function.

Renal impairment

• If you have renal impairment (kidney problems), use hyoscyamine with caution.
• Kidney function is essential for drug elimination from the body, and adjustments may be needed in individuals with impaired renal function.

Hyoscyamine: Drug Interaction

Risk Factor C (Monitor therapy)
Acetylcholinesterase Inhibitors	may reduce an anticholinergic agent's therapeutic impact. Acetylcholinesterase Inhibitors' therapeutic impact may be reduced by anticholinergic drugs.
Amantadine	may strengthen an anticholinergic agent's anticholinergic action.
Anticholinergic Agents	Other anticholinergic agents' negative or hazardous effects could be amplified.
Botulinum Toxin-Containing Products	may strengthen an anticholinergic agent's anticholinergic action.
Cannabinoid-Containing Products	Cannabinoid-containing products' tachycardic impact may be enhanced by anticholinergic agents. Exceptions: Cannabidiol.
Chloral Betaine	may worsen anticholinergic agents' harmful or hazardous effects.
Gastrointestinal Agents (Prokinetic)	The therapeutic benefit of gastrointestinal agents may be diminished by anticholinergic agents (Prokinetic).
Glucagon	Anticholinergic drugs may make glucagon's harmful or toxic effects worse. Particularly, there may be a higher chance of unfavorable gastrointestinal consequences.
Itopride	Itopride's therapeutic impact may be diminished by anticholinergic drugs.
Mianserin	may strengthen an anticholinergic agent's anticholinergic action.
Mirabegron	Anticholinergic drugs may make Mirabegron's harmful or hazardous effects worse.
Nitroglycerin	Nitroglycerin absorption may be decreased by anticholinergic agents. Anticholinergic medications specifically have the potential to impede or prevent the absorption of nitroglycerin by reducing the breakdown of sublingual nitroglycerin pills.
Opioid Agonists	Anticholinergic drugs may make opioid agonists more harmful or toxic. In particular, this combination may raise the risk of constipation and bladder retention.
Ramosetron	Ramosetron's tendency to cause constipation may be increased by anticholinergic drugs.
Thiazide and Thiazide-Like Diuretics	Thiazide and Thiazide-Like Diuretics can be found at higher concentrations in the serum when anticholinergic agents are used.
Topiramate	Topiramate's harmful or toxic effects may be increased by anticholinergic agents.
Risk Factor D (Consider therapy modification)
Antacids	may lower the level of hyoscyamine in the blood. In the event that both medications are taken together, treat the condition by giving instant-release hyoscyamine before meals and antacids after.
Pramlintide	may strengthen an anticholinergic agent's anticholinergic action. The GI tract alone is the target of these effects.
Secretin	The therapeutic impact of Secretin may be diminished by anticholinergic agents. Management: Prevent using secretin and anticholinergic medications together. At least five half-lives should pass before stopping anticholinergic medications in order to administer secretin.
Risk Factor X (Avoid combination)
Aclidinium	may strengthen an anticholinergic agent's anticholinergic action.
Cimetropium	The anticholinergic activity of cimetropium may be strengthened by anticholinergic agents.
Eluxadoline	Eluxadoline's constipating effects may be enhanced by anticholinergic drugs.
Glycopyrrolate (Oral Inhalation)	The anticholinergic action of glycopyrrolate may be enhanced by anticholinergic agents (Oral Inhalation).
Glycopyrronium (Topical)	might make anticholinergic agents more effective in blocking cholinergic receptors.
Ipratropium (Oral Inhalation)	Possibly makes anticholinergic agents more effective.
Levosulpiride	Levosulpiride's therapeutic impact may be diminished by anticholinergic medications.
Oxatomide	May strengthen an anticholinergic agent's anticholinergic action.
Potassium Chloride	Potassium chloride may have a stronger ulcerogenic impact when used with anticholinergic drugs. Treatment: Patients taking medications with strong anticholinergic effects should refrain from taking potassium chloride in any solid oral dose form.
Potassium Citrate	Potassium Citrate has an ulcerogenic action that may be enhanced by anticholinergic drugs.
Revefenacin	Revefenacin's anticholinergic action may be strengthened by anticholinergic agents.
Tiotropium	Tiotropium's anticholinergic action may be strengthened by anticholinergic drugs.
Umeclidinium	might make anticholinergic agents more effective in blocking cholinergic receptors.

Monitoring Parameters:

None mentioned.

How to administer Hyoscyamine?

Oral Formulations:

Elixir (Hyosyne):

• Recommended to take before meals (about 30 to 60 minutes) for gastrointestinal disorders.
• Administration before meals is suggested but not mandatory.

Drops (Hyosyne):

• Take before meals (about 30 to 60 minutes) for gastrointestinal disorders.
• Use the provided dropper to measure the dose accurately.

Regular Release Tablet (Levsin, Oscimin):

• Recommended to take before meals (about 30 to 60 minutes) for gastrointestinal disorders.

Dispersible Tablet:

• Recommended to take before meals (about 30 to 60 minutes) for gastrointestinal disorders.
• Anaspaz: Tablets may be used sublingually, chewed, or swallowed whole.
• Ed-Spaz: Dissolve on top of the tongue and swallow with saliva.
• NuLev, Oscimin: Tablets may be chewed or placed on the tongue and allowed to disintegrate.

Extended-Release Tablet:

• Recommended to take before meals (about 30 to 60 minutes) for gastrointestinal disorders.
• Levbid: Do not crush or chew.
• Oscimin SR, Symax Duotab, Symax SR: Swallow whole.

Sublingual Tablet:

• Recommended to take before meals (about 30 to 60 minutes) for gastrointestinal disorders.
• Levsin/SL: Tablets may be used sublingually, chewed, or swallowed whole.
• Symax SL: Tablets may be used sublingually or swallowed whole.
• Oscimin: Administer sublingually.

Injections:

IM (Intramuscular):

• May be administered without dilution.

IV (Intravenous):

• Inject over at least 1 minute.
• May be administered without dilution.

SubQ (Subcutaneous):

• May be administered without dilution.

Mechanism of action of Hyoscyamine:

• Hyoscyamine works by blocking the action of acetylcholine at certain points in the body's parasympathetic nervous system.
• This action occurs in smooth muscles, secretory glands, and the central nervous system (CNS).
• The effects of hyoscyamine include an increase in cardiac (heart) output, reduction in secretions (drying effect), and antagonism (blocking) of histamine and serotonin, which are chemical messengers in the body.

Timing of Effects:

• Onset of Action: Takes about 2 to 3 minutes for the effects to start.

Duration of Effects:

• Regular Release: Lasts for 4 to 6 hours.
• Extended Release (Levbid, Symax Duotab): Effects can last for 8 to 12 hours.

Body Processes:

• Absorption: Gets into the bloodstream well.
• Metabolism: Processed by the liver.
• Half-life Elimination:
  • Regular Release: Lasts in the body for 2 to 3.5 hours.
  • Extended Release (Levbid): Lasts in the body for approximately 7 hours.

Elimination:

• Excretion: Leaves the body through urine.

International Brand Names of Hyoscyamine:

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

Hyoscyamine Brand Names in Pakistan:

Hyoscyamine Drops 125 mcg/ml in Pakistan
Anapaz	Hilton Pharma (Pvt) Limited
Dosapaz	Dosaco Laboratories
Pan Calm	Imco Pharmaceuticals Laboratories

 

Hyoscyamine Tablets 125 mcg in Pakistan
Anapaz	Hilton Pharma (Pvt) Limited

 

Hyoscyamine Tablets 250 mcg in Pakistan
Acupaz	Glitz Pharma

 

Hyoscyamine Tablets DS 250 mcg in Pakistan
Anapaz	Hilton Pharma (Pvt) Limited