Acetylcholine

JFDA label: Miochol-E

Mechanism of Action

Causes contraction of the sphincter muscles of the iris, resulting in miosis and contraction of the ciliary muscle, leading to accommodation spasm

Indications

Approved

• Ophthalmic surgery

Contraindications

Source: Lexicomp

• Hypersensitivity to acetylcholine chloride or any component of the formulation Absolute

Adverse Reactions

Cardiac disorders (3)

Not Known Bradycardia · flushing · hypotension

Skin and subcutaneous tissue disorders (1)

Not Known Diaphoresis

Eye disorders (3)

Not Known Cloudy vision · corneal decompensation · corneal edema

Respiratory, thoracic and mediastinal disorders (1)

Not Known Dyspnea

Dosing

Source: Lexicomp

Warnings & Precautions

Source: Lexicomp

Diseases affected by systemic effects

Systemic effects rarely occur but can cause problems for patients with asthma, GI spasm, acute heart failure, hyperthyroidism, Parkinson's disease, peptic ulcer disease, and or urinary tract obstruction. In a scientific statement from the American Heart Association, ophthalmic cholinergic agents have been determined to be agents that may exacerbate underlying myocardial dysfunction (magnitude: minor) (AHA [Page 2016]). Other warnings/precautions:

Aseptic conditions

Open under aseptic conditions only; do not gas sterilize.

Cataract surgery

During cataract surgery, use only after lens is in place.

Pregnancy & Lactation

Chemistry & Properties

Formula	C7H16NO2+
Molecular weight	146.21 g/mol
IUPAC name	2-acetyloxyethyl(trimethyl)azanium
CAS	51-84-3
PubChem CID	187
InChIKey	OIPILFWXSMYKGL-UHFFFAOYSA-N
logP	0.26 (XLogP 0.2)
Polar surface area	26.3 Ų
H-bond acceptors / donors	2 / 0
Drug-likeness (QED)	0.42
Lipinski violations	0

SMILES

CC(=O)OCC[N+](C)(C)C

Biology & Pharmacokinetics

Pharmacokinetics predicted

Bioavailability	70.0%
Half-life	1.725 h
Volume of distribution	0.723 L/kg
Protein binding	4.1%
BBB penetrant	No

Enzyme interactions

Enzyme	Role	Detail
CYP1A2	Substrate	—
CYP2D6	Substrate	—

Receptor binding (top 6)

Target	Action	Affinity
Cholinergic, muscarinic M1 (CHRM1)	Binding	pKi 8.4
Cholinergic, Nicotinic Alpha4Beta2	Binding	pKi 8.2
Cholinergic, muscarinic M2 (CHRM2)	Binding	pKi 7.4
Cholinergic, muscarinic M3 (CHRM3)	Binding	pKi 6.9
Cholinergic, muscarinic M5 (CHRM5)	Binding	pKi 6.1
Cholinergic, muscarinic M4 (CHRM4)	Binding	pKi 5.3

Transporters

BCRP (Inhibitor)BSEP (Inhibitor)BSEP (Inhibitor)MRP1 (Inhibitor)OATP1B1 (Inhibitor)OATP1B3 (Inhibitor)OCT1 (Inhibitor)OCT2 (Inhibitor)OCTN1 (Inhibitor)P-gp (Inhibitor)OCT1 (Substrate)OCT2 (Substrate)OCT3 (Substrate)P-gp (Substrate)

Drug–drug interactions (43, DDInter)

Interacting drug	Severity	Management
Aclidinium	moderate
Acrivastine	moderate
Alimemazine	moderate
Atropine	moderate
Atropine (ophthalmic)	moderate
Azatadine	moderate
Brompheniramine	moderate
Carbinoxamine	moderate
Chlorcyclizine	moderate
Chlorpheniramine	moderate
Clemastine	moderate
Clidinium	moderate
Cyclizine	moderate
Cyproheptadine	moderate
Dexbrompheniramine	moderate
Dicyclomine	moderate
Diphenhydramine	moderate
Doxepin	moderate
Doxepin (topical)	moderate
Doxylamine	moderate
Glycopyrronium	moderate
Glycopyrronium (topical)	moderate
Hyoscyamine	moderate
Ipratropium	moderate
Meclizine	moderate
Mepenzolate	moderate
Mepyramine	moderate
Methdilazine	moderate
Methscopolamine	moderate
Phenindamine	moderate
Promethazine	moderate
Propantheline	moderate
Revefenacin	moderate
Scopolamine	moderate
Scopolamine (ophthalmic)	moderate
Thiethylperazine	moderate
Tiotropium	moderate
Tripelennamine	moderate
Triprolidine	moderate
Trospium	moderate

Showing 40 of 43.

Registered Products (1)

Brand	Form / strength	Pack	Agent	Citizen (JOD)
Miochol-E	Ampoule 20 mg/2 ml	1 amp	Petra Drug Store	—