Phil Pharmawealth/Atlantic Adrenaline

Adrenaline acid tartrate.

Each mL contains: Adrenaline (as Acid Tartrate) 1 mg.

Pharmacology: Pharmacokinetics: As a result of enzymatic degradation in the gut and first-pass metabolism in the liver, adrenaline is almost totally inactive when given orally. Systemic absorption can occur after topical application for example of eye drops. Adrenaline acts rapidly after intramuscular and subcutaneous injection; the latter route is, however, sometimes considered to be slower and therefore less reliable for emergency use. Although absorption is slowed by local vasoconstriction it can be hastened by massaging the injection site.
Most adrenaline that is either injected into the body or released into the circulation from the adrenal medulla is very rapidly inactivated by processes that include uptake into the adrenergic neurons, diffusion, and enzymatic degradation in the liver and body tissues. The half-life of circulating adrenaline is only about 1 minute. One of the enzymes responsible for the chemical inactivation of adrenaline is catechol-O-methyltransferase (COMT), the other is monoamine oxidase (MAO). In general, adrenaline is methylated to metanephrine by COMT followed by oxidative deamination by MAO and eventual conversion to 4-hydroxy-3-methoxymandelic acid (formerly termed vanillylmandelic acid; VMA), or oxidatively deaminated by MAO and converted to 3,4-dihydroxymandelic acid which, in turn, is methylated by COMT, once again to 4-hydroxy-3-methoxymandelic acid; the metabolites are excreted in the urine mainly as their glucuronide and ethereal sulfate conjugates.
The ability of COMT to effect introduction of a methyl group is an important step in the chemical inactivation of adrenaline and similar catecholamines (in particular, noradrenaline). It means that the termination of the pharmacological response of catecholamines is not simply dependent upon MAO. In its role of neurotransmitter intraneuronal catecholamine (mainly noradrenaline) is, however, enzymatically regulated by MAO.
Adrenaline crosses the placenta to enter fetal circulation.

Adrenaline has an important role in the management of acute allergic reactions and can be life-saving in patients with anaphylaxis and anaphylactic shock. It is also used in advanced cardiac life support. Adrenaline has been used in the treatment of acute asthma but more selective drugs are available, and it has no role in the chronic management of asthma. It has been given by nebulisation in severe group. Adrenaline is used for a number of other indications including the control of minor bleeding from the skin and mucous membranes, in ophthalmology chiefly for the management of open-angle (simple) glaucoma, and also as an adjunct to local anaesthesia.

The usual dose of adrenaline in anaphylactic shock is 500 micrograms (0.5 mL of a 1 in 1000 solution) by intramuscular injection repeated as necessary every 5 minutes. A dose of 300 micrograms (0.3 mL of a 1 in 1000 solution) may be appropriate for emergency self-administration, for example by autoinjector. The dose for children depends on age and weight, but is usually about 10 micrograms/kg by intramuscular injection. Suitable doses are 50 micrograms for infants under 6 months of age, 120 micrograms for children aged 6 months to 6 years, and 250 micrograms for those aged 6 to 12 years. If autoinjectors are used, a dose of 150 micrograms may be used for children weighing between 15 to 30 kg and 300 micrograms for those weighing over 30 kg. If intravenous administration is required the dose is 500 micrograms for adults and 10 micrograms/kg for children, given as a more dilute 1 in 10000 solution at a rate of 1 mL (100 micrograms) or less per minute.
In advanced cardiac life support the initial dose of adrenaline for adults is 1 mg intravenously (10 mL of a 1 in 10000 solution) and this may be repeated as often as every 2 to 3 minutes throughout the resuscitation procedure. The dose for children is 10 micrograms/kg intravenously. Higher intravenous doses have been used in both adults and children for the second and subsequent doses but are no longer generally recommended. Intraosseous doses for adults and children are the same as those used intravenously. Endotracheal doses for adults are 2 to 3 times the intravenous dose; children may be given 100 micrograms/kg.
Adrenaline relaxes the bronchial musculature and has sometimes been injected subcutaneously or intramuscularly in the management of acute asthmatic attacks. However, in general, the use of adrenaline in asthma has been superseded by beta, agonists, such as salbutamol, which can alleviate bronchospasm with fewer effects on the heart. If adrenaline is to be used, the adult dose is 0.3 to 0.5 mL of a 1 in 1000 aqueous solution (300 to 500 micrograms); children have received 0.01 mL/kg (10 micrograms/kg) to a maximum of 0.5 mL (500 micrograms). Aqueous solutions with an adrenaline content equivalent to 1 in 100 have occasionally been used by inhalation as a spray to alleviate asthmatic attacks; these solution must never be confused with the weaker strength used for injection. Pressurised aerosols delivering metered doses equivalent to about 160 micrograms to 275 micrograms of adrenaline have also been used; adults have received 1 or 2 metered inhalations repeated, if necessary, after 3 hours.
Adrenaline is frequently added to local anaesthetics to retard diffusion and limit absorption, to prolong the duration of effect, and to lessen the danger of toxicity. A concentration of 1 in 200000 (5 micrograms/mL) is usually used; adrenaline should not be added when procedures involve digits, ears, nose, penis, or scrotum owing to the risk of ischaemic tissue necrosis. A concentration of up to 1 in 80000 (12.5 micrograms/mL) may be used in dental preparations where the total dose given is small.

Adrenaline is frequently used in emergency situations and any contraindications are therefore relative.
Adrenaline may delay the second stage of labour and some manufacturers recommend that it should not be used during this time.
Adrenaline eye drops are contra-indicated in angle-closure glaucoma unless an iridectomy has been carried out.

Adrenaline may delay the second stage of labour and some manufacturers recommend that it should not be used during this time.

Adrenaline is a potent sympathomimetic and may exhibit the adverse effects typical of both alpha- and beta-adrenoceptor stimulation. Adverse effects such as anxiety, dyspnoea, hyperglycaemia, restlessness, palpitations, tachycardia (sometimes with anginal pain), tremors, sweating, hypersalivation, weakness, dizziness, headache, and coldness of extremities may occur even with low doses. Since adrenaline does not readily cross the blood-brain barrier, its central effects may be largely a somatic response to its peripheral effects. Overdosage may cause cardiac arrhythmias and a sharp rise in blood pressure (sometimes leading to cerebral haemorrhage and pulmonary oedema); these effects may occur at normal dosage in susceptible subjects.
Adrenaline is a potent vasoconstrictor and gangrene may occur if adrenaline-containing local anaesthetic solutions are infiltrated into digits. Extravasation of parenterally administered similarly causes intense vasoconstriction, resulting in tissue necrosis and sloughing.

Adrenaline has direct alpha- and beta-agonist actions and its interactions are complex and may be hazardous. Particular caution is needed if adrenaline is given to patients taking beta blockers since severe hypertension may result; the response to adrenaline in patients with anaphylaxis may also be impaired.

Store at temperatures not exceeding 30°C.

Cardiac Drugs

C01CA24 - epinephrine ; Belongs to the class of adrenergic and dopaminergic cardiac stimulants excluding glycosides. Used in the treatment of hypotension.

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