Details
Stereochemistry | RACEMIC |
Molecular Formula | C19H28NO3.C7H7O3S.H2O |
Molecular Weight | 507.639 |
Optical Activity | ( + / - ) |
Defined Stereocenters | 2 / 3 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
O.CC1=CC=C(C=C1)S([O-])(=O)=O.C[N+]2(C)CC[C@@H](C2)OC(=O)[C@@](O)(C3CCCC3)C4=CC=CC=C4
InChI
InChIKey=UOWOLENSDISMPG-FFUVTKDNSA-M
InChI=1S/C19H28NO3.C7H8O3S.H2O/c1-20(2)13-12-17(14-20)23-18(21)19(22,16-10-6-7-11-16)15-8-4-3-5-9-15;1-6-2-4-7(5-3-6)11(8,9)10;/h3-5,8-9,16-17,22H,6-7,10-14H2,1-2H3;2-5H,1H3,(H,8,9,10);1H2/q+1;;/p-1/t17-,19-;;/m0../s1
Molecular Formula | HO |
Molecular Weight | 17.0073 |
Charge | -1 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
Molecular Formula | C19H28NO3 |
Molecular Weight | 318.4305 |
Charge | 1 |
Count |
|
Stereochemistry | EPIMERIC |
Additional Stereochemistry | No |
Defined Stereocenters | 2 / 3 |
E/Z Centers | 0 |
Optical Activity | UNSPECIFIED |
Molecular Formula | C7H8O3S |
Molecular Weight | 172.202 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
Glycopyrrolate is a synthetic anticholinergic agent with a quaternary ammonium structure. Glycopyrrolate is a muscarinic competitive antagonist used as an antispasmodic, in some disorders of the gastrointestinal tract, and to reduce salivation with some anesthetics. Glycopyrrolate binds competitively to the muscarinic acetylcholine receptor. Like other anticholinergic (antimuscarinic) agents, it inhibits the action of acetylcholine on structures innervated by postganglionic cholinergic nerves and on smooth muscles that respond to acetylcholine but lack cholinergic innervation. These peripheral cholinergic receptors are present in the autonomic effector cells of smooth muscle, cardiac muscle, the sinoatrial node, the atrioventricular node, exocrine glands and, to a limited degree, in the autonomic ganglia. Thus, it diminishes the volume and free acidity of gastric secretions and controls excessive pharyngeal, tracheal, and bronchial secretions. Glycopyrrolate antagonizes muscarinic symptoms (e.g., bronchorrhea, bronchospasm, bradycardia, and
intestinal hypermotility) induced by cholinergic drugs such as the anticholinesterases.
The highly polar quaternary ammonium group of glycopyrrolate limits its passage across lipid
membranes, such as the blood-brain barrier, in contrast to atropine sulfate and scopolamine
hydrobromide, which are highly non-polar tertiary amines which penetrate lipid barriers easily. Glycopyrrolate is marketed under the brand names Robinul, Robinul Forte, Cuvposa. In October 2015, glycopyrrolate was approved by the FDA for use as a standalone treatment for Chronic obstructive pulmonary disease (COPD), as Seebri Neohaler.
Originator
Sources: http://adisinsight.springer.com/drugs/800042720
Curator's Comment: It was developed by Sosei and licensed to Novartis in 2005.
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
9.9 null [pIC50] | |||
9.3 null [pIC50] | |||
9.6 null [pIC50] | |||
9.8 null [pIC50] | |||
9.7 null [pIC50] | |||
Target ID: CHEMBL216 Sources: https://www.ncbi.nlm.nih.gov/pubmed/21036043 |
9.9 null [pIC50] | ||
Target ID: CHEMBL211 Sources: https://www.ncbi.nlm.nih.gov/pubmed/21036043 |
9.3 null [pIC50] | ||
Target ID: CHEMBL245 Sources: https://www.ncbi.nlm.nih.gov/pubmed/21036043 |
9.6 null [pIC50] | ||
Target ID: CHEMBL1821 Sources: https://www.ncbi.nlm.nih.gov/pubmed/21036043 |
9.8 null [pIC50] | ||
Target ID: CHEMBL2035 Sources: https://www.ncbi.nlm.nih.gov/pubmed/21036043 |
9.7 null [pIC50] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Sources: https://www.drugs.com/pro/robinul.html |
Primary | ROBINUL Approved UseFor use as adjunctive therapy in the treatment of peptic ulcer. Launch Date1961 |
||
Primary | SEEBRI NEOHALER Approved UseSEEBRI NEOHALER is an anticholinergic indicated for the long-term,
maintenance treatment of airflow obstruction in patients with chronic
obstructive pulmonary disease (COPD) Launch Date2015 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
0.08 ng/mL |
2.4 % 1 times / day multiple, topical dose: 2.4 % route of administration: Topical experiment type: MULTIPLE co-administered: |
GLYCOPYRRONIUM plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
3.47 μg/L |
8 μg/kg bw single, intravenous dose: 8 μg/kg bw route of administration: Intravenous experiment type: SINGLE co-administered: |
GLYCOPYRRONIUM plasma | Homo sapiens population: UNKNOWN age: ADULT sex: UNKNOWN food status: UNKNOWN |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
0.88 ng × h/mL |
2.4 % 1 times / day multiple, topical dose: 2.4 % route of administration: Topical experiment type: MULTIPLE co-administered: |
GLYCOPYRRONIUM plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
8.64 μg × h/L |
6 μg/kg bw single, intravenous dose: 6 μg/kg bw route of administration: Intravenous experiment type: SINGLE co-administered: |
GLYCOPYRRONIUM plasma | Homo sapiens population: UNKNOWN age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
6.64 μg × h/L |
8 μg/kg bw single, intravenous dose: 8 μg/kg bw route of administration: Intravenous experiment type: SINGLE co-administered: |
GLYCOPYRRONIUM plasma | Homo sapiens population: UNKNOWN age: ADULT sex: UNKNOWN food status: UNKNOWN |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
0.83 h |
6 μg/kg bw single, intravenous dose: 6 μg/kg bw route of administration: Intravenous experiment type: SINGLE co-administered: |
GLYCOPYRRONIUM plasma | Homo sapiens population: UNKNOWN age: ADULT sex: UNKNOWN food status: UNKNOWN |
Funbound
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
68.3% |
GLYCOPYRRONIUM plasma | Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
Doses
Dose | Population | Adverse events |
---|---|---|
2.4 % 1 times / day multiple, topical Recommended Dose: 2.4 %, 1 times / day Route: topical Route: multiple Dose: 2.4 %, 1 times / day Sources: |
unhealthy, 9 to 76 years Health Status: unhealthy Age Group: 9 to 76 years Sex: M+F Sources: |
Other AEs: Erythema, Burning sensation... Other AEs: Erythema (grade 1-2, 17%) Sources: Burning sensation (grade 1-2, 14.1%) Pruritus (grade 1-2, 8.1%) |
2.4 % 1 times / day multiple, topical Recommended Dose: 2.4 %, 1 times / day Route: topical Route: multiple Dose: 2.4 %, 1 times / day Sources: |
unhealthy, 9 to 76 years Health Status: unhealthy Age Group: 9 to 76 years Sex: M+F Sources: |
Other AEs: Dry mouth, Mydriasis... Other AEs: Dry mouth (24.2%) Sources: Mydriasis (6.8%) Oropharyngeal pain (5.7%) Headache (5%) Urinary hesitation (3.5%) Vision blurred (3.5%) Nasal dryness (2.6%) Dry throat (2.6%) Dry eye (2.4%) Dry skin (2.2%) Constipation (2%) |
2.4 % 1 times / day multiple, topical Recommended Dose: 2.4 %, 1 times / day Route: topical Route: multiple Dose: 2.4 %, 1 times / day Sources: |
unhealthy, 9 to 76 years Health Status: unhealthy Age Group: 9 to 76 years Sex: M+F Sources: |
Other AEs: Urinary retention, Nausea... Other AEs: Urinary retention (1.5%) Sources: Nausea (1.3%) Pruritus (1.3%) Epistaxis (1.1%) Alanine aminotransferase increased (4.9%) White blood cell count decreased (6.6%) |
2 % 1 times / day multiple, topical Studied dose Dose: 2 %, 1 times / day Route: topical Route: multiple Dose: 2 %, 1 times / day Sources: |
unhealthy, >18 years of age Health Status: unhealthy Age Group: >18 years of age Sex: M+F Sources: |
Other AEs: Abnormal ECG... Other AEs: Abnormal ECG (grade 1, 0.6%) Sources: |
2.4 % 1 times / day multiple, topical Recommended Dose: 2.4 %, 1 times / day Route: topical Route: multiple Dose: 2.4 %, 1 times / day Sources: |
unhealthy, Mean age 33 years Health Status: unhealthy Age Group: Mean age 33 years Sex: M+F Sources: |
Other AEs: Application site pain, Dermatitis... Other AEs: Application site pain (grade 1-2, 6.4%) Sources: Dermatitis (grade 1-2, 3.8%) Pruritus (grade 1-2, 3.8%) Rash (grade 1-2, 3.8%) Erythema (grade 1-2, 2.4%) |
2.4 % 1 times / day multiple, topical Recommended Dose: 2.4 %, 1 times / day Route: topical Route: multiple Dose: 2.4 %, 1 times / day Sources: |
unhealthy, Mean age 33 years Health Status: unhealthy Age Group: Mean age 33 years Sex: M+F Sources: |
Other AEs: Dry mouth, Vision blurred... Other AEs: Dry mouth (16.9%) Sources: Vision blurred (6.7%) Nasopharyngitis (5.8%) Mydriasis (5.3%) Urinary hesitation (4.2%) Nasal dryness (3.6%) Dry eye (2.9%) Pharyngitis (2.2%) |
2.4 % 1 times / day multiple, topical Recommended Dose: 2.4 %, 1 times / day Route: topical Route: multiple Dose: 2.4 %, 1 times / day Sources: |
unhealthy, Mean age 33 years Health Status: unhealthy Age Group: Mean age 33 years Sex: M+F Sources: |
Disc. AE: Vision blurred, Dry mouth... AEs leading to discontinuation/dose reduction: Vision blurred (grade 1-2, 1.8%) Sources: Dry mouth (grade 1-2, 1.6%) Application site dermatitis (grade 1-2, 0.9%) Urinary hesitation (grade 1-2, 0.9%) |
4 % 1 times / day steady, topical Highest studied dose Dose: 4 %, 1 times / day Route: topical Route: steady Dose: 4 %, 1 times / day Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sex: M+F Sources: |
|
2.4 % 1 times / day multiple, topical Studied dose Dose: 2.4 %, 1 times / day Route: topical Route: multiple Dose: 2.4 %, 1 times / day Sources: |
unhealthy, mean age 20.4 years Health Status: unhealthy Age Group: mean age 20.4 years Sex: M+F Sources: |
Other AEs: Headache, Cough... Other AEs: Headache (grade 1, 12.9%) Sources: Cough (grade 1, 3.2%) Laceration (grade 1, 3.2%) Rhinorrhea (grade 1, 3.2%) |
2 mg 2 times / day multiple, oral Studied dose Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: |
unhealthy, mean age 33 years Health Status: unhealthy Age Group: mean age 33 years Sex: M+F Sources: |
Disc. AE: Xerostomia, Erectile dysfunction... Other AEs: Dry mouth... AEs leading to discontinuation/dose reduction: Xerostomia (12.5%) Other AEs:Erectile dysfunction (4.2%) Headaches (4.2%) Urinary retention (4.2%) Dry mouth (50%) Sources: |
3 mg 3 times / day multiple, oral Studied dose Dose: 3 mg, 3 times / day Route: oral Route: multiple Dose: 3 mg, 3 times / day Sources: |
healthy, mean age 44 years Health Status: healthy Age Group: mean age 44 years Sex: M+F Sources: |
Other AEs: Dry mouth, Headache... Other AEs: Dry mouth (grade 1, 16.7%) Sources: Headache (grade 1, 5.6%) Nocturia (grade 1, 11.1%) Chest pain (grade 1, 5.6%) Hypoesthesia (grade 1, 5.6%) Nasal dryness (grade 1, 5.6%) |
2.4 % 1 times / day multiple, topical Recommended Dose: 2.4 %, 1 times / day Route: topical Route: multiple Dose: 2.4 %, 1 times / day Sources: |
unhealthy, median age 31 years Health Status: unhealthy Age Group: median age 31 years Sex: M+F Sources: |
Disc. AE: Dry mouth, Retention urinary... AEs leading to discontinuation/dose reduction: Dry mouth (grade 1-2, 1.1%) Sources: Retention urinary (grade 1-2, 0.9%) Urinary hesitation (grade 1-2, 0.7%) Vision blurred (grade 1-2, 0.4%) |
2.4 % 6 times / day single, topical Studied dose Dose: 2.4 %, 6 times / day Route: topical Route: single Dose: 2.4 %, 6 times / day Sources: |
unhealthy Health Status: unhealthy Sources: |
Other AEs: Urinary hesitation, Vision blurred... Other AEs: Urinary hesitation Sources: Vision blurred Dry mouth Application site erythema Dry throat Dry eye Nasal dryness |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Burning sensation | grade 1-2, 14.1% | 2.4 % 1 times / day multiple, topical Recommended Dose: 2.4 %, 1 times / day Route: topical Route: multiple Dose: 2.4 %, 1 times / day Sources: |
unhealthy, 9 to 76 years Health Status: unhealthy Age Group: 9 to 76 years Sex: M+F Sources: |
Erythema | grade 1-2, 17% | 2.4 % 1 times / day multiple, topical Recommended Dose: 2.4 %, 1 times / day Route: topical Route: multiple Dose: 2.4 %, 1 times / day Sources: |
unhealthy, 9 to 76 years Health Status: unhealthy Age Group: 9 to 76 years Sex: M+F Sources: |
Pruritus | grade 1-2, 8.1% | 2.4 % 1 times / day multiple, topical Recommended Dose: 2.4 %, 1 times / day Route: topical Route: multiple Dose: 2.4 %, 1 times / day Sources: |
unhealthy, 9 to 76 years Health Status: unhealthy Age Group: 9 to 76 years Sex: M+F Sources: |
Constipation | 2% | 2.4 % 1 times / day multiple, topical Recommended Dose: 2.4 %, 1 times / day Route: topical Route: multiple Dose: 2.4 %, 1 times / day Sources: |
unhealthy, 9 to 76 years Health Status: unhealthy Age Group: 9 to 76 years Sex: M+F Sources: |
Dry skin | 2.2% | 2.4 % 1 times / day multiple, topical Recommended Dose: 2.4 %, 1 times / day Route: topical Route: multiple Dose: 2.4 %, 1 times / day Sources: |
unhealthy, 9 to 76 years Health Status: unhealthy Age Group: 9 to 76 years Sex: M+F Sources: |
Dry eye | 2.4% | 2.4 % 1 times / day multiple, topical Recommended Dose: 2.4 %, 1 times / day Route: topical Route: multiple Dose: 2.4 %, 1 times / day Sources: |
unhealthy, 9 to 76 years Health Status: unhealthy Age Group: 9 to 76 years Sex: M+F Sources: |
Dry throat | 2.6% | 2.4 % 1 times / day multiple, topical Recommended Dose: 2.4 %, 1 times / day Route: topical Route: multiple Dose: 2.4 %, 1 times / day Sources: |
unhealthy, 9 to 76 years Health Status: unhealthy Age Group: 9 to 76 years Sex: M+F Sources: |
Nasal dryness | 2.6% | 2.4 % 1 times / day multiple, topical Recommended Dose: 2.4 %, 1 times / day Route: topical Route: multiple Dose: 2.4 %, 1 times / day Sources: |
unhealthy, 9 to 76 years Health Status: unhealthy Age Group: 9 to 76 years Sex: M+F Sources: |
Dry mouth | 24.2% | 2.4 % 1 times / day multiple, topical Recommended Dose: 2.4 %, 1 times / day Route: topical Route: multiple Dose: 2.4 %, 1 times / day Sources: |
unhealthy, 9 to 76 years Health Status: unhealthy Age Group: 9 to 76 years Sex: M+F Sources: |
Urinary hesitation | 3.5% | 2.4 % 1 times / day multiple, topical Recommended Dose: 2.4 %, 1 times / day Route: topical Route: multiple Dose: 2.4 %, 1 times / day Sources: |
unhealthy, 9 to 76 years Health Status: unhealthy Age Group: 9 to 76 years Sex: M+F Sources: |
Vision blurred | 3.5% | 2.4 % 1 times / day multiple, topical Recommended Dose: 2.4 %, 1 times / day Route: topical Route: multiple Dose: 2.4 %, 1 times / day Sources: |
unhealthy, 9 to 76 years Health Status: unhealthy Age Group: 9 to 76 years Sex: M+F Sources: |
Headache | 5% | 2.4 % 1 times / day multiple, topical Recommended Dose: 2.4 %, 1 times / day Route: topical Route: multiple Dose: 2.4 %, 1 times / day Sources: |
unhealthy, 9 to 76 years Health Status: unhealthy Age Group: 9 to 76 years Sex: M+F Sources: |
Oropharyngeal pain | 5.7% | 2.4 % 1 times / day multiple, topical Recommended Dose: 2.4 %, 1 times / day Route: topical Route: multiple Dose: 2.4 %, 1 times / day Sources: |
unhealthy, 9 to 76 years Health Status: unhealthy Age Group: 9 to 76 years Sex: M+F Sources: |
Mydriasis | 6.8% | 2.4 % 1 times / day multiple, topical Recommended Dose: 2.4 %, 1 times / day Route: topical Route: multiple Dose: 2.4 %, 1 times / day Sources: |
unhealthy, 9 to 76 years Health Status: unhealthy Age Group: 9 to 76 years Sex: M+F Sources: |
Epistaxis | 1.1% | 2.4 % 1 times / day multiple, topical Recommended Dose: 2.4 %, 1 times / day Route: topical Route: multiple Dose: 2.4 %, 1 times / day Sources: |
unhealthy, 9 to 76 years Health Status: unhealthy Age Group: 9 to 76 years Sex: M+F Sources: |
Nausea | 1.3% | 2.4 % 1 times / day multiple, topical Recommended Dose: 2.4 %, 1 times / day Route: topical Route: multiple Dose: 2.4 %, 1 times / day Sources: |
unhealthy, 9 to 76 years Health Status: unhealthy Age Group: 9 to 76 years Sex: M+F Sources: |
Pruritus | 1.3% | 2.4 % 1 times / day multiple, topical Recommended Dose: 2.4 %, 1 times / day Route: topical Route: multiple Dose: 2.4 %, 1 times / day Sources: |
unhealthy, 9 to 76 years Health Status: unhealthy Age Group: 9 to 76 years Sex: M+F Sources: |
Urinary retention | 1.5% | 2.4 % 1 times / day multiple, topical Recommended Dose: 2.4 %, 1 times / day Route: topical Route: multiple Dose: 2.4 %, 1 times / day Sources: |
unhealthy, 9 to 76 years Health Status: unhealthy Age Group: 9 to 76 years Sex: M+F Sources: |
Alanine aminotransferase increased | 4.9% | 2.4 % 1 times / day multiple, topical Recommended Dose: 2.4 %, 1 times / day Route: topical Route: multiple Dose: 2.4 %, 1 times / day Sources: |
unhealthy, 9 to 76 years Health Status: unhealthy Age Group: 9 to 76 years Sex: M+F Sources: |
White blood cell count decreased | 6.6% | 2.4 % 1 times / day multiple, topical Recommended Dose: 2.4 %, 1 times / day Route: topical Route: multiple Dose: 2.4 %, 1 times / day Sources: |
unhealthy, 9 to 76 years Health Status: unhealthy Age Group: 9 to 76 years Sex: M+F Sources: |
Abnormal ECG | grade 1, 0.6% | 2 % 1 times / day multiple, topical Studied dose Dose: 2 %, 1 times / day Route: topical Route: multiple Dose: 2 %, 1 times / day Sources: |
unhealthy, >18 years of age Health Status: unhealthy Age Group: >18 years of age Sex: M+F Sources: |
Erythema | grade 1-2, 2.4% | 2.4 % 1 times / day multiple, topical Recommended Dose: 2.4 %, 1 times / day Route: topical Route: multiple Dose: 2.4 %, 1 times / day Sources: |
unhealthy, Mean age 33 years Health Status: unhealthy Age Group: Mean age 33 years Sex: M+F Sources: |
Dermatitis | grade 1-2, 3.8% | 2.4 % 1 times / day multiple, topical Recommended Dose: 2.4 %, 1 times / day Route: topical Route: multiple Dose: 2.4 %, 1 times / day Sources: |
unhealthy, Mean age 33 years Health Status: unhealthy Age Group: Mean age 33 years Sex: M+F Sources: |
Pruritus | grade 1-2, 3.8% | 2.4 % 1 times / day multiple, topical Recommended Dose: 2.4 %, 1 times / day Route: topical Route: multiple Dose: 2.4 %, 1 times / day Sources: |
unhealthy, Mean age 33 years Health Status: unhealthy Age Group: Mean age 33 years Sex: M+F Sources: |
Rash | grade 1-2, 3.8% | 2.4 % 1 times / day multiple, topical Recommended Dose: 2.4 %, 1 times / day Route: topical Route: multiple Dose: 2.4 %, 1 times / day Sources: |
unhealthy, Mean age 33 years Health Status: unhealthy Age Group: Mean age 33 years Sex: M+F Sources: |
Application site pain | grade 1-2, 6.4% | 2.4 % 1 times / day multiple, topical Recommended Dose: 2.4 %, 1 times / day Route: topical Route: multiple Dose: 2.4 %, 1 times / day Sources: |
unhealthy, Mean age 33 years Health Status: unhealthy Age Group: Mean age 33 years Sex: M+F Sources: |
Dry mouth | 16.9% | 2.4 % 1 times / day multiple, topical Recommended Dose: 2.4 %, 1 times / day Route: topical Route: multiple Dose: 2.4 %, 1 times / day Sources: |
unhealthy, Mean age 33 years Health Status: unhealthy Age Group: Mean age 33 years Sex: M+F Sources: |
Pharyngitis | 2.2% | 2.4 % 1 times / day multiple, topical Recommended Dose: 2.4 %, 1 times / day Route: topical Route: multiple Dose: 2.4 %, 1 times / day Sources: |
unhealthy, Mean age 33 years Health Status: unhealthy Age Group: Mean age 33 years Sex: M+F Sources: |
Dry eye | 2.9% | 2.4 % 1 times / day multiple, topical Recommended Dose: 2.4 %, 1 times / day Route: topical Route: multiple Dose: 2.4 %, 1 times / day Sources: |
unhealthy, Mean age 33 years Health Status: unhealthy Age Group: Mean age 33 years Sex: M+F Sources: |
Nasal dryness | 3.6% | 2.4 % 1 times / day multiple, topical Recommended Dose: 2.4 %, 1 times / day Route: topical Route: multiple Dose: 2.4 %, 1 times / day Sources: |
unhealthy, Mean age 33 years Health Status: unhealthy Age Group: Mean age 33 years Sex: M+F Sources: |
Urinary hesitation | 4.2% | 2.4 % 1 times / day multiple, topical Recommended Dose: 2.4 %, 1 times / day Route: topical Route: multiple Dose: 2.4 %, 1 times / day Sources: |
unhealthy, Mean age 33 years Health Status: unhealthy Age Group: Mean age 33 years Sex: M+F Sources: |
Mydriasis | 5.3% | 2.4 % 1 times / day multiple, topical Recommended Dose: 2.4 %, 1 times / day Route: topical Route: multiple Dose: 2.4 %, 1 times / day Sources: |
unhealthy, Mean age 33 years Health Status: unhealthy Age Group: Mean age 33 years Sex: M+F Sources: |
Nasopharyngitis | 5.8% | 2.4 % 1 times / day multiple, topical Recommended Dose: 2.4 %, 1 times / day Route: topical Route: multiple Dose: 2.4 %, 1 times / day Sources: |
unhealthy, Mean age 33 years Health Status: unhealthy Age Group: Mean age 33 years Sex: M+F Sources: |
Vision blurred | 6.7% | 2.4 % 1 times / day multiple, topical Recommended Dose: 2.4 %, 1 times / day Route: topical Route: multiple Dose: 2.4 %, 1 times / day Sources: |
unhealthy, Mean age 33 years Health Status: unhealthy Age Group: Mean age 33 years Sex: M+F Sources: |
Application site dermatitis | grade 1-2, 0.9% Disc. AE |
2.4 % 1 times / day multiple, topical Recommended Dose: 2.4 %, 1 times / day Route: topical Route: multiple Dose: 2.4 %, 1 times / day Sources: |
unhealthy, Mean age 33 years Health Status: unhealthy Age Group: Mean age 33 years Sex: M+F Sources: |
Urinary hesitation | grade 1-2, 0.9% Disc. AE |
2.4 % 1 times / day multiple, topical Recommended Dose: 2.4 %, 1 times / day Route: topical Route: multiple Dose: 2.4 %, 1 times / day Sources: |
unhealthy, Mean age 33 years Health Status: unhealthy Age Group: Mean age 33 years Sex: M+F Sources: |
Dry mouth | grade 1-2, 1.6% Disc. AE |
2.4 % 1 times / day multiple, topical Recommended Dose: 2.4 %, 1 times / day Route: topical Route: multiple Dose: 2.4 %, 1 times / day Sources: |
unhealthy, Mean age 33 years Health Status: unhealthy Age Group: Mean age 33 years Sex: M+F Sources: |
Vision blurred | grade 1-2, 1.8% Disc. AE |
2.4 % 1 times / day multiple, topical Recommended Dose: 2.4 %, 1 times / day Route: topical Route: multiple Dose: 2.4 %, 1 times / day Sources: |
unhealthy, Mean age 33 years Health Status: unhealthy Age Group: Mean age 33 years Sex: M+F Sources: |
Headache | grade 1, 12.9% | 2.4 % 1 times / day multiple, topical Studied dose Dose: 2.4 %, 1 times / day Route: topical Route: multiple Dose: 2.4 %, 1 times / day Sources: |
unhealthy, mean age 20.4 years Health Status: unhealthy Age Group: mean age 20.4 years Sex: M+F Sources: |
Cough | grade 1, 3.2% | 2.4 % 1 times / day multiple, topical Studied dose Dose: 2.4 %, 1 times / day Route: topical Route: multiple Dose: 2.4 %, 1 times / day Sources: |
unhealthy, mean age 20.4 years Health Status: unhealthy Age Group: mean age 20.4 years Sex: M+F Sources: |
Laceration | grade 1, 3.2% | 2.4 % 1 times / day multiple, topical Studied dose Dose: 2.4 %, 1 times / day Route: topical Route: multiple Dose: 2.4 %, 1 times / day Sources: |
unhealthy, mean age 20.4 years Health Status: unhealthy Age Group: mean age 20.4 years Sex: M+F Sources: |
Rhinorrhea | grade 1, 3.2% | 2.4 % 1 times / day multiple, topical Studied dose Dose: 2.4 %, 1 times / day Route: topical Route: multiple Dose: 2.4 %, 1 times / day Sources: |
unhealthy, mean age 20.4 years Health Status: unhealthy Age Group: mean age 20.4 years Sex: M+F Sources: |
Xerostomia | 12.5% Disc. AE |
2 mg 2 times / day multiple, oral Studied dose Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: |
unhealthy, mean age 33 years Health Status: unhealthy Age Group: mean age 33 years Sex: M+F Sources: |
Erectile dysfunction | 4.2% Disc. AE |
2 mg 2 times / day multiple, oral Studied dose Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: |
unhealthy, mean age 33 years Health Status: unhealthy Age Group: mean age 33 years Sex: M+F Sources: |
Headaches | 4.2% Disc. AE |
2 mg 2 times / day multiple, oral Studied dose Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: |
unhealthy, mean age 33 years Health Status: unhealthy Age Group: mean age 33 years Sex: M+F Sources: |
Urinary retention | 4.2% Disc. AE |
2 mg 2 times / day multiple, oral Studied dose Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: |
unhealthy, mean age 33 years Health Status: unhealthy Age Group: mean age 33 years Sex: M+F Sources: |
Dry mouth | 50% | 2 mg 2 times / day multiple, oral Studied dose Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: |
unhealthy, mean age 33 years Health Status: unhealthy Age Group: mean age 33 years Sex: M+F Sources: |
Nocturia | grade 1, 11.1% | 3 mg 3 times / day multiple, oral Studied dose Dose: 3 mg, 3 times / day Route: oral Route: multiple Dose: 3 mg, 3 times / day Sources: |
healthy, mean age 44 years Health Status: healthy Age Group: mean age 44 years Sex: M+F Sources: |
Dry mouth | grade 1, 16.7% | 3 mg 3 times / day multiple, oral Studied dose Dose: 3 mg, 3 times / day Route: oral Route: multiple Dose: 3 mg, 3 times / day Sources: |
healthy, mean age 44 years Health Status: healthy Age Group: mean age 44 years Sex: M+F Sources: |
Chest pain | grade 1, 5.6% | 3 mg 3 times / day multiple, oral Studied dose Dose: 3 mg, 3 times / day Route: oral Route: multiple Dose: 3 mg, 3 times / day Sources: |
healthy, mean age 44 years Health Status: healthy Age Group: mean age 44 years Sex: M+F Sources: |
Headache | grade 1, 5.6% | 3 mg 3 times / day multiple, oral Studied dose Dose: 3 mg, 3 times / day Route: oral Route: multiple Dose: 3 mg, 3 times / day Sources: |
healthy, mean age 44 years Health Status: healthy Age Group: mean age 44 years Sex: M+F Sources: |
Hypoesthesia | grade 1, 5.6% | 3 mg 3 times / day multiple, oral Studied dose Dose: 3 mg, 3 times / day Route: oral Route: multiple Dose: 3 mg, 3 times / day Sources: |
healthy, mean age 44 years Health Status: healthy Age Group: mean age 44 years Sex: M+F Sources: |
Nasal dryness | grade 1, 5.6% | 3 mg 3 times / day multiple, oral Studied dose Dose: 3 mg, 3 times / day Route: oral Route: multiple Dose: 3 mg, 3 times / day Sources: |
healthy, mean age 44 years Health Status: healthy Age Group: mean age 44 years Sex: M+F Sources: |
Vision blurred | grade 1-2, 0.4% Disc. AE |
2.4 % 1 times / day multiple, topical Recommended Dose: 2.4 %, 1 times / day Route: topical Route: multiple Dose: 2.4 %, 1 times / day Sources: |
unhealthy, median age 31 years Health Status: unhealthy Age Group: median age 31 years Sex: M+F Sources: |
Urinary hesitation | grade 1-2, 0.7% Disc. AE |
2.4 % 1 times / day multiple, topical Recommended Dose: 2.4 %, 1 times / day Route: topical Route: multiple Dose: 2.4 %, 1 times / day Sources: |
unhealthy, median age 31 years Health Status: unhealthy Age Group: median age 31 years Sex: M+F Sources: |
Retention urinary | grade 1-2, 0.9% Disc. AE |
2.4 % 1 times / day multiple, topical Recommended Dose: 2.4 %, 1 times / day Route: topical Route: multiple Dose: 2.4 %, 1 times / day Sources: |
unhealthy, median age 31 years Health Status: unhealthy Age Group: median age 31 years Sex: M+F Sources: |
Dry mouth | grade 1-2, 1.1% Disc. AE |
2.4 % 1 times / day multiple, topical Recommended Dose: 2.4 %, 1 times / day Route: topical Route: multiple Dose: 2.4 %, 1 times / day Sources: |
unhealthy, median age 31 years Health Status: unhealthy Age Group: median age 31 years Sex: M+F Sources: |
Application site erythema | 2.4 % 6 times / day single, topical Studied dose Dose: 2.4 %, 6 times / day Route: topical Route: single Dose: 2.4 %, 6 times / day Sources: |
unhealthy Health Status: unhealthy Sources: |
|
Dry eye | 2.4 % 6 times / day single, topical Studied dose Dose: 2.4 %, 6 times / day Route: topical Route: single Dose: 2.4 %, 6 times / day Sources: |
unhealthy Health Status: unhealthy Sources: |
|
Dry mouth | 2.4 % 6 times / day single, topical Studied dose Dose: 2.4 %, 6 times / day Route: topical Route: single Dose: 2.4 %, 6 times / day Sources: |
unhealthy Health Status: unhealthy Sources: |
|
Dry throat | 2.4 % 6 times / day single, topical Studied dose Dose: 2.4 %, 6 times / day Route: topical Route: single Dose: 2.4 %, 6 times / day Sources: |
unhealthy Health Status: unhealthy Sources: |
|
Nasal dryness | 2.4 % 6 times / day single, topical Studied dose Dose: 2.4 %, 6 times / day Route: topical Route: single Dose: 2.4 %, 6 times / day Sources: |
unhealthy Health Status: unhealthy Sources: |
|
Urinary hesitation | 2.4 % 6 times / day single, topical Studied dose Dose: 2.4 %, 6 times / day Route: topical Route: single Dose: 2.4 %, 6 times / day Sources: |
unhealthy Health Status: unhealthy Sources: |
|
Vision blurred | 2.4 % 6 times / day single, topical Studied dose Dose: 2.4 %, 6 times / day Route: topical Route: single Dose: 2.4 %, 6 times / day Sources: |
unhealthy Health Status: unhealthy Sources: |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
OverviewOther
Other Inhibitor | Other Substrate | Other Inducer |
---|---|---|
Drug as perpetrator
Drug as victim
PubMed
Title | Date | PubMed |
---|---|---|
Excess tachycardia: heart rate after antimuscarinic agents in conscious dogs. | 1984 Feb |
|
Effect of halogenated anaesthetics on heart rate changes during reversal of neuromuscular block with glycopyrrolate and neostigmine. | 1984 Nov |
|
Comparison of i.v. glycopyrrolate and atropine in the prevention of bradycardia and arrhythmias following repeated doses of suxamethonium in children. | 1984 Sep |
|
Effects of oral potassium supplements on upper gastrointestinal mucosa: multicenter clinical comparison of three formulations and placebo. | 1986 |
|
Refractory bradycardia after reversal of muscle relaxant in a diabetic with vagal neuropathy. | 1986 Nov |
|
Twelve-hour bronchodilation in asthma with a single aerosol dose of the anticholinergic compound glycopyrrolate. | 1988 Jul |
|
A glycopyrrolate-ritodrine drug-drug interaction. | 1988 Mar |
|
Glycopyrronium requirements for antagonism of the muscarinic side effects of edrophonium. | 1989 Jan |
|
Sensitivity to both vecuronium and neostigmine in a sero-negative myasthenic patient. | 1989 Oct |
|
Attenuation of vagal reflexes during tracheal intubation following vagotonic anesthetic agents. | 1994 Oct |
|
Urinary retention caused by topical glycopyrrolate for hyperhidrosis. | 2006 Sep |
|
Comparing the cardiovascular therapeutic indices of glycopyrronium and tiotropium in an integrated rat pharmacokinetic, pharmacodynamic and safety model. | 2015 Aug 15 |
Sample Use Guides
In Vivo Use Guide
Sources: https://www.drugs.com/dosage/glycopyrrolate.html
Curator's Comment: Can be used as inhalation powder, for oral inhalation for the long-term,
maintenance treatment of airflow obstruction in patients with chronic
obstructive pulmonary disease (COPD) use https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/207923lbl.pdf
Usual Adult Dose for Anesthesia
Preanesthetic (reduction of secretions): 0.004 mg (0.02 mL)/kg IM 30 to 60 minutes prior to the anticipated time of induction of anesthesia or at the time the preanesthetic narcotic and/or sedative are administered.
Intraoperative: 0.1 mg (0.5 mL) IV repeated as needed every 2 to 3 minutes.
Reversal of neuromuscular blockade: 0.2 mg (1.0 mL) IV for each 1.0 mg of neostigmine or 5 mg of pyridostigmine.
Reversal of bradycardia, vagal reflexes (intraoperative): 0.1 mg IV repeated as needed at 2 to 3 minute intervals.
Usual Adult Dose for Peptic Ulcer
Parenteral: 0.1 mg (0.5 mL) IV or IM every 4 hours, 3 to 4 times daily. If a more profound effect is required the dose may be increased to 0.2 mg (1 mL).
1 mg oral tablet:
Initial dose: 1 mg orally 3 times daily or 1 mg in the morning, 1 mg in the early afternoon, and 2 mg at bedtime.
Maintenance dose: 1 mg orally twice daily to a maximum of 8 mg per day.
2 mg oral tablet: 2 mg orally 2 to 3 times daily to a maximum of 8 mg per day.
1.5 mg oral tablet: Used to provide intermediate titration doses based on patient response.
Usual Pediatric Dose for Anesthesia
Preanesthetic: 0.004 mg (0.02 mL)/kg IM 30 to 60 minutes prior to the anticipated time of induction of anesthesia or at the time the preanesthetic narcotic and/or sedative are administered. Children under 2 years of age may require up to 0.009 mg (0.45 mL)/kg.
Intraoperative: 0.004 mg (0.02 mL)/kg IV not to exceed 0.1 mg (0.5 mL) in a single dose, repeated as needed every 2 to 3 minutes.
Reversal of neuromuscular blockade: 0.4 mg (2 mL)/kg IV for each 1 mg of neostigmine or 5 mg of pyridostigmine.
Reversal of bradycardia, vagal reflexes (intraoperative): 4 mcg/kg/dose IV (maximum dose: 100 mcg/dose) at 2 to 3 minute intervals.
Usual Pediatric Dose for Excessive Salivation
3 years to 16 years with neurologic conditions associated with problem drooling:
Initiate dosing at 0.02 mg/kg orally three times daily and titrate in increments of 0.02 mg/kg every 5 to 7 days, based on therapeutic response and adverse reactions. Maximum recommended dose is 0.1 mg/kg three times daily, not to exceed 1.5 to 3 mg per dose based upon weight. Administer at least one hour before or two hours after meals.
Route of Administration:
Other
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/10385241
Glycopyrrolate inhibited contraction induced by EFS
(40 V, 0.5 ms, 4 Hz for 15 s every 4 min) in guinea-pig trachea
in a concentration-dependent manner (IC50=0.15 nM, n=5 ±
12). Glycopyrrolate inhibited contraction induced by EFS
(40 V, 0.5 ms, 8 Hz for 15 s every 4 min) in human trachea in
a concentration-dependent manner (IC50=0.44 nM, n=3 ± 8).
Substance Class |
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