ALMOTAN 6.25

Indications

• Acute treatment of migraine attacks with or without aura in adults

Dosage

Children: Almotriptan is not licensed for use in children or adolescents under 18 years of age.

Adults: For adults, the recommended dose is 12.5 mg to be taken as soon as possible after the onset of a migraine, followed by an additional 12.5 mg after 2 hours if necessary. The maximum dosage should not exceed 25 mg per day.

Mechanism of action

Almotriptan binds with high affinity to human 5-HT1B and 5-HT1D receptors, leading to cranial blood vessel constriction. This agonist activity correlates with the relief of migraine headache, as it also activates 5-HT1 receptors on peripheral terminals of the trigeminal nerve innervating cranial blood vessels, contributing to its antimigraine effects.

Pharmacodynamics

Almotriptan is a selective 5-HT receptor agonist that specifically targets the 5-HT1B and 5-HT1D subtypes. Its action leads to vasoconstriction of cranial blood vessels and may also involve modulation of trigeminal nerve activity. This pharmacological profile is effective in treating acute migraine attacks but does not extend to long-term prophylactic use.

Pharmacokinetics

Almotriptan is absorbed after oral administration, reaching peak plasma concentrations within approximately 1.5 to 2 hours. It undergoes hepatic metabolism primarily via cytochrome P450 enzymes, with a half-life of around 3 to 4 hours. Renal excretion is the primary route for elimination of its metabolites.

Contra-indications

• Arrhythmias
• Coronary vasospasm
• Heart failure
• Ischaemic heart disease
• Peripheral vascular disease
• Previous cerebrovascular accident
• Previous myocardial infarction
• Previous transient ischaemic attack
• Prinzmetal’s angina
• Severe uncontrolled hypertension

Adverse effects

• Nausea
• Pain
• Palpitations
• Throat tightness
• Vertigo
• Agitation
• Decreased appetite
• Arthralgia
• Constipation
• Gastrointestinal disorders
• Hyperbilirubinaemia
• Lymphadenopathy
• Menorrhagia

Interactions

• Cobicistat may increase exposure to Almotriptan
• Idelalisib may increase exposure to Almotriptan
• Clarithromycin may increase exposure to Almotriptan
• Almotriptan and ergotamine may increase the risk of vasoconstriction

Precautions

• Caution in patients with conditions predisposing to coronary artery disease
• Caution in the elderly
• Monitor for symptoms of heat, heaviness, pressure, or tightness (including throat and chest)

Pregnancy

Limited experience with 5-HT1 receptor agonists during pregnancy; manufacturers advise avoidance unless potential benefits outweigh risks.

Breast-feeding

Present in milk in animal studies; avoid breastfeeding for 24 hours.

Storage

Store at room temperature, away from light and moisture.

Formulations

• Tablets, 12.5 mg and 25 mg

Indications

• Support in energy metabolism
• Management of metabolic disorders
• Potential role in exercise performance enhancement

Dosage

Children: Refer to specific guidance in the BNF for Children.

Adults: Refer to specific guidance in the BNF.

Mechanism of action

Malate participates in the malate-aspartate shuttle, which is essential for transferring reducing equivalents across the mitochondrial membrane. This shuttle allows for the conversion of NADH produced during glycolysis to NADH within the mitochondria, thus facilitating ATP production. Additionally, malate is involved in gluconeogenesis, where it contributes to the synthesis of glucose from non-carbohydrate precursors.

Pharmacodynamics

Malate aids in energy metabolism, particularly in the conversion of nutrients to ATP. It supports the regeneration of NAD+, which is crucial for numerous metabolic reactions. By participating in the TCA cycle, malate enhances aerobic respiration and plays a role in maintaining the balance of metabolic intermediates necessary for cellular function.

Pharmacokinetics

Malate is readily absorbed in the gastrointestinal tract and is distributed throughout the body, where it enters various metabolic pathways. It is primarily metabolized in the liver and muscle tissues. The elimination of malate is through metabolic conversion, with its metabolites being further processed in the TCA cycle.

Pregnancy

There are no well-controlled studies of malate in pregnant women. Use only if clearly needed.

Breast-feeding

Malate is considered to be safe during breastfeeding, though limited data are available.

Storage

Store in a cool, dry place away from direct sunlight. Keep out of reach of children.

Formulations

• Malate salts
• Malic acid

Mechanism of action

Almotriptan binds with high affinity to human 5-HT_1B and 5-HT_1D receptors leading to cranial blood vessel constriction.

Pharmacodynamics

Almotriptan is a selective 5-hydroxytryptamine receptor subtype agonist indicated for the acute treatment of migraine attacks with or without aura in adults. Almotriptan is not intended for the prophylactic therapy of migraine or for use in the management of hemiplegic or basilar migraine. Almotriptan is an agonist for a vascular 5-hydroxytryptamine receptor subtype (probably a member of the 5-HT_1D family) having only a weak affinity for 5-HT_1A, 5-HT_5A, and 5-HT₇ receptors and no significant affinity or pharmacological activity at 5-HT₂, 5-HT₃ or 5-HT₄ receptor subtypes or at alpha1-, alpha2-, or beta-adrenergic, dopamine1,; dopamine2; muscarinic, or benzodiazepine receptors. This action in humans correlates with the relief of migraine headache. In addition to causing vasoconstriction, experimental data from animal studies show that Almotriptan also activates 5-HT₁ receptors on peripheral terminals of the trigeminal nerve innervating cranial blood vessels, which may also contribute to the antimigrainous effect of Almotriptan in humans.