Bellergal Spacetabs

Bellergal Spacetabs Uses, Dosage, Side Effects, Food Interaction and all others data.

Belladonna, also known as atropa belladonna or deadly nightshade, is a perennial herbaceous plant in the nightshade family Solanaceae. Its roots, leaves and fruits contain Hyoscyamine, Scopolamine, and mostly, Atropine. These alkaloids are naturally-occurring muscarinic antagonists. Atropine is a non-selective muscarinic antagonist that is mainly used as an adjunct for anaesthesia. The name "belladonna" originates from the Italian words "beautiful woman" and the historical use of herb eye-drops by women to dilate the pupils of the eyes for aesthetic purposes. Belladonna is a poisonous plant and belladonna intoxication from accidental ingestion may result in a severe anticholinergic syndrome, which is associated with both central and peripheral manifestations .

The active components of belladonna mediate anticholinergic actions. The main effects include inhibition of secretions such as dry mouth, tachycardia, pupillary dilation and paralysis of accommodation, relaxation of smooth muscles in the gut, bronchi, biliary tract and bladder (urinary retention), and inhibition of gastric acid secretion . Atropine is a stimulant of the central nervous system .

A vasoconstrictor found in ergot of Central Europe. It is an alpha-1 selective adrenergic agonist and is commonly used in the treatment of migraine disorders.

Ergotamine is a vasoconstrictor and alpha adrenoreceptor antagonist. The pharmacological properties of ergotamine are extremely complex; some of its actions are unrelated to each other, and even mutually antagonistic. The drug has partial agonist and/or antagonist activity against tryptaminergic, dopaminergic and alpha adrenergic receptors depending upon their site, and it is a highly active uterine stimulant. It causes constriction of peripheral and cranial blood vessels and produces depression of central vasomotor centers. The pain of a migraine attack is believed to be due to greatly increased amplitude of pulsations in the cranial arteries, especially the meningeal branches of the external carotid artery. Ergotamine reduces extracranial blood flow, causes a decline in the amplitude of pulsation in the cranial arteries, and decreases hyperperfusion of the territory of the basilar artery. It does not reduce cerebral hemispheric blood flow.

Phenobarbital is a long-acting barbiturate. It depresses the sensory cortex, reduces motor activity, changes cerebellar function and produces drowsiness, sedation and hypnosis. Its anticonvulsant property is exhibited at high doses.

Phenobarbital acts on GABAA receptors, increasing synaptic inhibition. This has the effect of elevating seizure threshold and reducing the spread of seizure activity from a seizure focus. Phenobarbital may also inhibit calcium channels, resulting in a decrease in excitatory transmitter release. The sedative-hypnotic effects of phenobarbital are likely the result of its effect on the polysynaptic midbrain reticular formation, which controls CNS arousal.

Phenobarbital, the longest-acting barbiturate, is used for its anticonvulsant and sedative-hypnotic properties in the management of all seizure disorders except absence (petit mal).

Trade Name Bellergal Spacetabs
Generic belladonna + ergotamine + phenobarbital
Type
Therapeutic Class
Manufacturer
Available Country Canada, United States
Last Updated: September 19, 2023 at 7:00 am
Bellergal Spacetabs
Bellergal Spacetabs

Uses

No therapeutic indications.

Ergotamine is a alpha-1 selective adrenergic agonist vasoconstrictor used to treat migraines with or without aura and cluster headaches.

For use as therapy to abort or prevent vascular headache, e.g., migraine, migraine variants, or so called "histaminic cephalalgia".

Phenobarbital is used as-

  • Sedative and hence it relieves anxiety, tension and fear
  • Hypnotic and hence it is used for short term insomnia
  • Pre-anaesthetics
  • Anti-epileptic in epilepsy with Partial seizure or Generalized Tonic-clonic seizure, status epilepticus
  • Certain acute convulsive episodes

Bellergal Spacetabs is also used to associated treatment for these conditions: Acid Reflux, Bloating, Heartburn, Menopausal Symptoms, Poisoning of the Intestine, Poisoning of the Stomach, Belching, Gastrointestinal spasmsCluster Headache, Migraine, Uterine Atony, Vascular HeadachesAlcohol Withdrawal Syndrome, Anxiety, Febrile Convulsions, Hyperbilirubinemia, Insomnia, Menopausal Symptoms, Partial-Onset Seizures, Withdrawal Symptoms, Generalized seizure, Sedation

How Bellergal Spacetabs works

The active components of belladonna act as competitive antagonists at muscarinic receptors and block the binding of acetylcholine to the central nervous system and parasympathetic postganglionic muscarinic receptors .

Ergotamine acts on migraine by one of two proposed mechanisms: 1) activation of 5-HT1D receptors located on intracranial blood vessels, including those on arterio-venous anastomoses, leads to vasoconstriction, which correlates with the relief of migraine headache, and 2) activation of 5-HT1D receptors on sensory nerve endings of the trigeminal system results in the inhibition of pro-inflammatory neuropeptide release.

Phenobarbital acts on GABAA receptors, increasing synaptic inhibition. This has the effect of elevating seizure threshold and reducing the spread of seizure activity from a seizure focus. Phenobarbital may also inhibit calcium channels, resulting in a decrease in excitatory transmitter release. The sedative-hypnotic effects of phenobarbital are likely the result of its effect on the polysynaptic midbrain reticular formation, which controls CNS arousal.

Dosage

Bellergal Spacetabs dosage

Adults:

  • Hypnosis: 100 to 320 mg
  • Sedation: 30 to 120 mg/day in 2 to 3 divided doses
  • Epilepsy: 60 to 250 mg/day
  • Convulsion: 50 to 100 mg/day in 2 to 3 divided doses
  • Status epilepticus: IV 10-20 mg/Kg, repeat if needed

Children:

  • Preoperative: 1-3 mg/Kg body weight
  • Convulsion: 4-6 mg/Kg/day
  • Status epilepticus: IV 15-20 mg/Kg over 10-15 minutes

Dilute with most IV infusion soln (e.g. NaCl 0.45% or 0.9%, lactated Ringer's, dextrose 5%, Ringer's).

Side Effects

Drowsiness is the most common side effect. Less common side effects are CNS depression, nervousness, agitation, psychiatric disturbance, lethargy, mental depression, ataxia, nightmares, bradycardia, apnea, nausea, vomiting, constipation, restlessness and confusion in the elderly and hyperkinesia in children.

Toxicity

Oral LD50 of atropine is 75 mg/kg in mouse. Clinical manifestations of anticholinergic syndrome include both central and peripheral effects. Central symptoms, which are dose-dependent and anticholinergic agent-specific, include ataxia, disorientation, short-term memory loss, confusion, hallucinations, psychosis, agitated delirium, seizures, coma, respiratory failure or cardiovascular collapse . Peripheral effects include mydriasis with cycloplegia, dry mucous membranes, hyperreflexia, flushed skin, diminished bowel sounds or ileus, urinary retention, tachycardia, and hypertension or hypotension . Management of anticholinergic intoxication should be symptomatic including gastrointestinal decontamination with activated charcoal . The antidote for belladonna poisoning is Physostigmine, which is the same as for atropine . Physosigmine crosses the blood-brain barrier and reversibly inhibits anticholinesterase. Benzodiazepines are frequently used for sedation to control anticholinergic effects including delirium and agitation .

Signs of overexposure include irritation, nausea, vomiting, headache, diarrhea, thirst, coldness of skin, pruritus, weak pulse, numbness, tingling of extremities, and confusion.

CNS and respiratory depression which may progress to Cheyne-Stokes respiration, areflexia, constriction of the pupils to a slight degree (though in severe poisoning they may wshow paralytic dilation), oliguria, tachycardia, hypotension, lowered body temperature, and coma. Typical shock syndrome (apnea, circulatory collapse, respiratory arrest, and death) may occur.

Precaution

Phenobarbital is potentially habit forming if taken over an extended period of time. When being prescribed to overcome insomnia, the drug should not be used for a period longer than two weeks. Caution should be taken in patients who are mentally depressed, have hepatic damage, suicidal tendencies or a history of drug abuse.

Interaction

Phenobarbital can interact with a number of prescription and nonprescription medications including acetaminophen, anticoagulants such as warfarin, chloramphenicol, monoamine oxidase inhibitors (MAOIs), antidepressants, asthma medicine, cold medicine, anti-allergy medicine, sedatives, steroids, tranquilizers, and vitamins. Interactions with these medications can increase the drowsiness caused by phenobarbital.

Volume of Distribution

For pharmacokinetic information of the active ingredients, refer to Atropine, Hyoscyamine, or Scopolamine.

Elimination Route

For pharmacokinetic information of the active ingredients, refer to Atropine, Hyoscyamine, or Scopolamine.

The bioavailability of sublingually administered ergotamine has not been determined.

Absorbed in varying degrees following oral, rectal or parenteral administration. The salts are more rapidly absorbed than are the acids. The rate of absorption is increased if the sodium salt is ingested as a dilute solution or taken on an empty stomach.

Half Life

For pharmacokinetic information of the active ingredients, refer to Atropine, Hyoscyamine, or Scopolamine.

2 hours

53 to 118 hours (mean 79 hours)

Clearance

For pharmacokinetic information of the active ingredients, refer to Atropine, Hyoscyamine, or Scopolamine.

Elimination Route

For pharmacokinetic information of the active ingredients, refer to Atropine, Hyoscyamine, or Scopolamine.

Pregnancy & Breastfeeding use

Pregnancy Category D. Phenobarbital can cause potential fetal damage. Their use in pregnancy alone, or in combination with other anticonvulsants, can cause coagulation defects in the newborn infant which may be preventable by the prophylactic administration of Vitamin K to the mother prior to delivery. Phenobarbital is excreted through human milk; so caution should be taken during lactation period.

Contraindication

Phenobarbital is contraindicated in patients with acute intermittent porphyria and who have a natural or idiosyncrasy to barbiturates

Special Warning

Debilitated patient: Reduce dose

Renal Impairment: Reduce dose. Severe: Contraindicated

Hepatic Impairment: Reduce dose. Severe: Contraindicated

Acute Overdose

Phenobarbital should not be used more than the dosage guide line. 1 gm Phenobarbital oral dose may cause serious poisoning and 2 gm may cause even death. Over dosage produces severe, persistent depression. Treatment includes artificial respiration, maintenance of fluid balance and antibiotics to prevent pneumonia. Alkalinisation of the urine and forced diuresis or haemodialysis have been used in cases of severe poisoning.

Storage Condition

Protect from light, store in cool and dry place. Keep out of reach of children.

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