Atropine is a naturally occurring phytochemical alkaloid, originally identified in Atropa belladonna, but found in many members of the Solanaceae family. The most common sources of this active pharmaceutical ingredient (API) are Atropa belladonna, Datura innoxia, D. metel, and D. stramonium, but it can also be obtained from members of the Brugmansia and Hyoscyamus genera.1 Natural elixirs containing atropine were used for millennia, often in combination with opium, as an anesthetic to be administrated before surgery or cautery.1 The use of these natural elixirs was later replaced by the use of isolated active ingredients.2-4 The first total synthesis of atropine was achieved by German Chemist Richard Willstätter in 1901.5 Currently, atropine is on the World Health Organization’s List of Essential Medicines.
C2 PHARMA is the leading manufacturer and supplier of atropine sulfate. It is synthesized chemically.
Atropine sulfate injections are used as an antidote to treat poisoning caused by cholinergic drugs, mushrooms, organophosphate pesticides and nerve gas. it is also used to increase temporarily heart rate or decrease AV-block until definitive intervention can take place, when bradycardia or AV-block are judged to be hemodynamically significant and thought to be due to excess vagal tone.
Atropine sulfate ophthalmic formulations (eye drops), are used topically as a cycloplegic pre-diagnostic agent to paralyze temporarily the ciliary muscle of the eye, resulting in a loss of accommodation reflex, and as a therapeutic mydriatic agent to dilate the pupils. Due to its mydriatic properties, atropine sulfate is used in the therapy of refractive and accommodative amblyopia (lazy eye disease), by inducing blur in the healthy eye.
Atropine Sulfate oral tabs are used as a general antiemetic agent to reduce cramps: spastic bladder, infant colic, renal and biliary colic, peptic ulcer, non-ulcer dyspepsia, diverticular disease and irritable bowel syndrome.
MECHANISM OF ACTION
Atropine is a racemic mixture of D- and L-hyoscyamine. It is commonly classified as an anticholinergic or antiparasympathetic (parasympatholytic) drug. It binds to muscarinic acetylcholine receptors types M1, M2, M3, M4 and M5, producing a wide range of anticholinergic effects.6 For this reason, atropine administration has an effect on the parasympathetic nervous system, regulating the activity of glands, like salivary and mucus glands. Due to its competitive-antagonism at muscarinic receptors, atropine inhibits acetylcholine activity, thus it is indicated in the treatment for poisoning caused by organophosphate insecticides and nerve gases, such as tabun, sarin, soman and VX. In the eye, atropine blocks the release of acetylcholine, diminishing the contraction of the circular pupillary sphincter muscle, which results in mydriasis. It also paralyzes the ciliary muscles causing cyclopegia.7
- Holzman, R.S. Anesthesiology.1998, 89, 241–249.
- Mein, H.F.G. Annalen der Pharmacie,1831, 6, 67–72.
- Geiger and Hesse. Annalen der Pharmacie,1833, 5, 43 –681.
- Geiger and Hesse. Annalen der Pharmacie,1833, 6, 44 –65.
- Willstätter, R. Berichte der Deutschen chemischen Gesellschaft zu Berlin 1901, 34, 3163 – 3165.
- Gyermek, L. In: Pharmacology of antimuscarinic agents, 1997, CRS press, p.57.
- Georgievski, Z.; Koklanis, K.; Leone, J. Clinical and Experimental Ophthalmology, 2008, 36, A764-A765.