Atropine is an antimuscarinic agent which competitively antagonises acetylcholine at postganglionic nerve endings, thus affecting receptors in the exocrine glands, smooth muscle, cardiac muscle and the central nervous system.

Peripheral effects include decreased production of saliva, sweat, nasal, lachrymal and gastric secretions, decreased intestinal motility and inhibition of micturition.

Atropine increases sinus rate and sinoatrial and AV conduction. Usually heart rate is increased, but there may be an initial bradycardia.

Atropine inhibits secretions throughout the respiratory tract and relaxes bronchial smooth muscle producing bronchodilation.
5.2 Pharmacokinetic properties
Absorption

Following intravenous administration, the peak increase in heart rate occurs within 2 to 4 minutes. Peak plasma concentrations of atropine after intramuscular administration are reached within 30 minutes, although peak effects on the heart, sweating and salivation may occur 1 hour after intramuscular administration.

Distribution

Plasma levels after intramuscular and intravenous injection are comparable at 1 hour. Atropine is distributed widely throughout the body and crosses the blood brain barrier and the placenta barrier.

Biotransformation

Atropine is incompletely metabolised in the liver and is excreted in the urine as unchanged drug and metabolites. About 50% of the dose is excreted within 4 hours and 90% in 24 hours.

Elimination

The elimination half-life is about 2 to 5 hours. Up to 50% of the dose is protein bound.

Paediatric Population

Children, particularly those younger than two years, may be more susceptible to the actions of atropine. The elimination half-life is more than doubled in children less than two years compared to adults.
Elderly

The elimination half-life of atropine is more than doubled in the elderly (>65 years old) compared to adults.
5.3 Preclinical safety data
Effects in non-clinical studies were observed only at exposures considered sufficiently in excess of the maximum human exposure indicating little relevance to clinical use.

Atropine sulfate reduced fertility in male rats, presumably as a consequence of an inhibitory effect on the transport of sperm and semen during the process of emission.

6. Pharmaceutical particulars
6.1 List of excipients
Sodium chloride

Concentrated hydrochloric acid (for pH adjustment)

Water for injections
6.2 Incompatibilities
This medicinal product must not be mixed with other medicinal products.
6.3 Shelf life
Unopened blister pack: 3 years
6.4 Special precautions for storage
This medicinal product does not require any special storage conditions.
6.5 Nature and contents of container
5 ml solution in a pre-filled syringe (polypropylene) without needle, individually packaged in a transparent blister, available in box of 1, 5, 10, 12 or 20.

Not all pack sizes may be marketed
6.6 Special precautions for disposal and other handling
Instructions for use:

Be careful to strictly respect the protocol for the use of the syringe.

The pre-filled syringe is for single patient only. Discard syringe after use. DO NOT REUSE.

The content of un-opened and un-damaged blister is sterile, and must not be opened until used.

The product should be inspected visually for particles and discoloration prior to administration. Only c