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hyoscyamine (Levbid, Levsin, Anaspaz, Cystospaz, NuLev, Symax Duotab)

 

Classes: Anticholinergic Agents

Dosing and uses of Levbid, Levsin (hyoscyamine)

 

Adult dosage forms and strengths

capsule/tablet, extended release

  • 0.375mg

elixir

  • 0.125mg/5mL

injection solution

  • 0.5mg/mL

oral drops

  • 0.125mg/mL

tablet

  • 0.125mg

 

Gastrointestinal Disorders

Immediate release: 0.125-0.25 mg PO/SL q4hr PRN; no more than 1.5 mg/day

Extended release: 0.375-0.75 mg PO q12hr; no more than 1.5 mg/day

IM/SC/IV: 0.25-0.5 mg q4hr PRN; no more than 4 times per day

 

Hypermotility of Lower Urinary Tract

Adjunctive treatment

Immediate release: 0.15-0.3 mg PO/SL q6hr

Extended release: 0.375 mg PO q12hr

 

Peptic Ulcer Disease

Adjunctive treatment

0.125-0.25 mg PO/SL q4hr PRN; no more than 1.5 mg/day

 

Irritable Bowel Syndrome

Adjunctive treatment

0.125-0.25 mg PO/SL q4hr PRN; no more than 1.5 mg/day

 

Pediatric dosage forms and strengths

capsule/tablet, extended release

  • 0.375mg

elixir

  • 0.125mg/5mL

injection solution

  • 0.5mg/mL

oral drops

  • 0.125mg/mL

tablet

  • 0.125mg

 

Gastrointestinal Disorders

<2 years (oral drops)

  • 2.3-3.3 kg: 3 drops PO q4hr PRN; no more than 18 drops/day
  • 3.4-4 kg: 4 drops PO q4hr PRN; no more than 24 drops/day
  • 5-6 kg: 5 drops PO q4hr PRN; no more than 30 drops/day
  • 7-9 kg: 6 drops PO q4hr PRN; no more than 36 drops/day
  • 10-14 kg: 8 drops PO q4hr PRN; no more than 48 drops/day
  • ≥15 kg: 11 drops PO q4hr PRN; no more than 66 drops/day

2-12 years (tablet)

  • Immediate release/SL: 0.0625-0.125 mg PO q4hr PRN; no more than 0.75mg/day
  • Extended release: 0.375 PO q12hr; no more than 0.75 mg/day

2-12 years (elixir)

  • 10-19 kg: 1/4 tsp (1.25 mL) PO q4hr PRN
  • 20-39 kg: 1/2 tsp (2.5 mL) PO q4hr PRN
  • 40-49 kg: 3/4 tsp (3.75 mL) PO q4hr PRN
  • ≥50 kg: 1 tsp (5 mL) PO q4hr PRN

IV/IM/SQ

  • >12 years: 0.025-0.5 mg q4hr PRN; no more than 4 times daily

 

Geriatric dosage forms and strengths

 

Hypermotility of lower urinary tract

Immediate release: 0.125-0.25 mg PO/SL q6hr

Extended release: 0.375 mg PO q12hr

 

Dosing considerations

Avoid except in short-term situations to decrease secretions; high incidence of anticholinergic effects (Beers criteria)

 

Levbid, Levsin (hyoscyamine) adverse (side) effects

>10%

Dry skin

 

1-10%

Blurred vision

Constipation

Dysphagia

Photosensitivity

 

<1%

Headache

Orthostatic hypotension

Tachycardia

 

Frequency not defined

Xerostomia

Urinary hesitancy/retention

HTn

Dysphagia

Respiratory depression

CNS stimulation

Fever

Ataxia

Excitation

Lethargy

Palpitations

Mydriasis

Cycloplegia

Increased IOp

Weakness

Bloated feeling

Suppression of lactation

Impotence

Anhidrosis

 

Warnings

Contraindications

Hypersensitivity to hyoscyamine or related compounds

Closed-angle glaucoma

Myasthenia gravis

Hemorrhage with cardiovascular instability

Paralytic ileus

Intestinal atony of elderly/debilitated patient

Obstructive uropathy

Toxic megacolon

GI obstruction

Tachycardia secondary to cardiac insufficiency or thyrotoxicosis

Breastfeeding

 

Cautions

Renal/hepatic impairment

BPH

CHF

Coronary artery disease

HTn

COPd

Hiatal hernia

Reflux esophagitis

Mitral stenosis

Brain damage or spastic paralysis in children

Salivary secretion disorder

Down syndrome

Autonomic neuropathy

Hyperthyroidism

Tachyarrhythmia

Toxin-mediated diarrhea

Elderly (see Beers criteria)

 

Pregnancy and lactation

Pregnancy category: C

Lactation: Enters breast milk; use not recommended

 

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 Levbid, Levsin (hyoscyamine)

Mechanism of action

Parasympatholytic, atropine-like effects, especially peripherally; blocks the action of acetylcholine at parasympathetic sites in smooth muscle, secretory glands, and CNs

 

Absorption

Bioavailability: Tab (100%), SR (81%)

Onset: IV/IM/SC (2-3 min), SL (5-20 min), tab/SR (20-30 min)

Duration: IV/IM/SC/tab/SL (up to 4 hr), SR (12 hr)

Peak plasma time: Tab/SR (2.5 hr)

 

Distribution

Protein bound: 50%

Vd: 1.2-1.9 L/kg (adults); 1.1-3.7 L/kg (children aged 4-16 years)

 

Metabolism

Hepatic

Metabolites: Tropic acid, tropine, hyoscyamine glucuronide

 

Elimination

Half-life: Tab (3.5 hr), SR (5-9 hr)

Dialyzable: Yes; removed by hemodialysis and peritoneal dialysis

Excretion: Majority excreted in urine as unchanged drug