Details
Stereochemistry | RACEMIC |
Molecular Formula | C19H28NO3.C7H7O3S |
Molecular Weight | 489.624 |
Optical Activity | ( + / - ) |
Defined Stereocenters | 2 / 2 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
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=OFNFMAIFGLDTDC-QQTWVUFVSA-M
InChI=1S/C19H28NO3.C7H8O3S/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)/q+1;/p-1/t17-,19-;/m0./s1
Molecular Formula | C7H7O3S |
Molecular Weight | 171.194 |
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 / 2 |
E/Z Centers | 0 |
Optical Activity | UNSPECIFIED |
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 |
|
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 |
|
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 |
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 n = 459 Health Status: unhealthy Condition: Axillary Hyperhidrosis Age Group: 9 to 76 years Sex: M+F Population Size: 459 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 n = 459 Health Status: unhealthy Condition: Axillary Hyperhidrosis Age Group: 9 to 76 years Sex: M+F Population Size: 459 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 n = 459 Health Status: unhealthy Condition: Axillary Hyperhidrosis Age Group: 9 to 76 years Sex: M+F Population Size: 459 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 (mean) Studied dose Dose: 2 %, 1 times / day Route: topical Route: multiple Dose: 2 %, 1 times / day Sources: |
unhealthy, >18 years of age n = 338 Health Status: unhealthy Condition: Axillary Hyperhidrosis Age Group: >18 years of age Sex: M+F Population Size: 338 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 n = 564 Health Status: unhealthy Condition: Axillary Hyperhidrosis Age Group: Mean age 33 years Sex: M+F Population Size: 564 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 n = 564 Health Status: unhealthy Condition: Axillary Hyperhidrosis Age Group: Mean age 33 years Sex: M+F Population Size: 564 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 n = 564 Health Status: unhealthy Condition: Axillary Hyperhidrosis Age Group: Mean age 33 years Sex: M+F Population Size: 564 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: Page: 145 |
unhealthy, adult n = 19 Health Status: unhealthy Condition: hyperhidrosis Age Group: adult Sex: M+F Population Size: 19 Sources: Page: 145 |
|
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 n = 31 Health Status: unhealthy Age Group: mean age 20.4 years Sex: M+F Population Size: 31 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 (typical) Studied dose Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: |
unhealthy, mean age 33 years n = 24 Health Status: unhealthy Condition: hyperhidrosis Age Group: mean age 33 years Sex: M+F Population Size: 24 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 (max) Studied dose Dose: 3 mg, 3 times / day Route: oral Route: multiple Dose: 3 mg, 3 times / day Sources: |
healthy, mean age 44 years n = 18 Health Status: healthy Age Group: mean age 44 years Sex: M+F Population Size: 18 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 n = 459 Health Status: unhealthy Condition: Axillary Hyperhidrosis Age Group: median age 31 years Sex: M+F Population Size: 459 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 n = 1 Health Status: unhealthy Condition: Axillary Hyperhidrosis Population Size: 1 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 n = 459 Health Status: unhealthy Condition: Axillary Hyperhidrosis Age Group: 9 to 76 years Sex: M+F Population Size: 459 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 n = 459 Health Status: unhealthy Condition: Axillary Hyperhidrosis Age Group: 9 to 76 years Sex: M+F Population Size: 459 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 n = 459 Health Status: unhealthy Condition: Axillary Hyperhidrosis Age Group: 9 to 76 years Sex: M+F Population Size: 459 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 n = 459 Health Status: unhealthy Condition: Axillary Hyperhidrosis Age Group: 9 to 76 years Sex: M+F Population Size: 459 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 n = 459 Health Status: unhealthy Condition: Axillary Hyperhidrosis Age Group: 9 to 76 years Sex: M+F Population Size: 459 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 n = 459 Health Status: unhealthy Condition: Axillary Hyperhidrosis Age Group: 9 to 76 years Sex: M+F Population Size: 459 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 n = 459 Health Status: unhealthy Condition: Axillary Hyperhidrosis Age Group: 9 to 76 years Sex: M+F Population Size: 459 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 n = 459 Health Status: unhealthy Condition: Axillary Hyperhidrosis Age Group: 9 to 76 years Sex: M+F Population Size: 459 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 n = 459 Health Status: unhealthy Condition: Axillary Hyperhidrosis Age Group: 9 to 76 years Sex: M+F Population Size: 459 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 n = 459 Health Status: unhealthy Condition: Axillary Hyperhidrosis Age Group: 9 to 76 years Sex: M+F Population Size: 459 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 n = 459 Health Status: unhealthy Condition: Axillary Hyperhidrosis Age Group: 9 to 76 years Sex: M+F Population Size: 459 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 n = 459 Health Status: unhealthy Condition: Axillary Hyperhidrosis Age Group: 9 to 76 years Sex: M+F Population Size: 459 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 n = 459 Health Status: unhealthy Condition: Axillary Hyperhidrosis Age Group: 9 to 76 years Sex: M+F Population Size: 459 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 n = 459 Health Status: unhealthy Condition: Axillary Hyperhidrosis Age Group: 9 to 76 years Sex: M+F Population Size: 459 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 n = 459 Health Status: unhealthy Condition: Axillary Hyperhidrosis Age Group: 9 to 76 years Sex: M+F Population Size: 459 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 n = 459 Health Status: unhealthy Condition: Axillary Hyperhidrosis Age Group: 9 to 76 years Sex: M+F Population Size: 459 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 n = 459 Health Status: unhealthy Condition: Axillary Hyperhidrosis Age Group: 9 to 76 years Sex: M+F Population Size: 459 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 n = 459 Health Status: unhealthy Condition: Axillary Hyperhidrosis Age Group: 9 to 76 years Sex: M+F Population Size: 459 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 n = 459 Health Status: unhealthy Condition: Axillary Hyperhidrosis Age Group: 9 to 76 years Sex: M+F Population Size: 459 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 n = 459 Health Status: unhealthy Condition: Axillary Hyperhidrosis Age Group: 9 to 76 years Sex: M+F Population Size: 459 Sources: |
Abnormal ECG | grade 1, 0.6% | 2 % 1 times / day multiple, topical (mean) Studied dose Dose: 2 %, 1 times / day Route: topical Route: multiple Dose: 2 %, 1 times / day Sources: |
unhealthy, >18 years of age n = 338 Health Status: unhealthy Condition: Axillary Hyperhidrosis Age Group: >18 years of age Sex: M+F Population Size: 338 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 n = 564 Health Status: unhealthy Condition: Axillary Hyperhidrosis Age Group: Mean age 33 years Sex: M+F Population Size: 564 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 n = 564 Health Status: unhealthy Condition: Axillary Hyperhidrosis Age Group: Mean age 33 years Sex: M+F Population Size: 564 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 n = 564 Health Status: unhealthy Condition: Axillary Hyperhidrosis Age Group: Mean age 33 years Sex: M+F Population Size: 564 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 n = 564 Health Status: unhealthy Condition: Axillary Hyperhidrosis Age Group: Mean age 33 years Sex: M+F Population Size: 564 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 n = 564 Health Status: unhealthy Condition: Axillary Hyperhidrosis Age Group: Mean age 33 years Sex: M+F Population Size: 564 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 n = 564 Health Status: unhealthy Condition: Axillary Hyperhidrosis Age Group: Mean age 33 years Sex: M+F Population Size: 564 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 n = 564 Health Status: unhealthy Condition: Axillary Hyperhidrosis Age Group: Mean age 33 years Sex: M+F Population Size: 564 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 n = 564 Health Status: unhealthy Condition: Axillary Hyperhidrosis Age Group: Mean age 33 years Sex: M+F Population Size: 564 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 n = 564 Health Status: unhealthy Condition: Axillary Hyperhidrosis Age Group: Mean age 33 years Sex: M+F Population Size: 564 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 n = 564 Health Status: unhealthy Condition: Axillary Hyperhidrosis Age Group: Mean age 33 years Sex: M+F Population Size: 564 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 n = 564 Health Status: unhealthy Condition: Axillary Hyperhidrosis Age Group: Mean age 33 years Sex: M+F Population Size: 564 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 n = 564 Health Status: unhealthy Condition: Axillary Hyperhidrosis Age Group: Mean age 33 years Sex: M+F Population Size: 564 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 n = 564 Health Status: unhealthy Condition: Axillary Hyperhidrosis Age Group: Mean age 33 years Sex: M+F Population Size: 564 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 n = 564 Health Status: unhealthy Condition: Axillary Hyperhidrosis Age Group: Mean age 33 years Sex: M+F Population Size: 564 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 n = 564 Health Status: unhealthy Condition: Axillary Hyperhidrosis Age Group: Mean age 33 years Sex: M+F Population Size: 564 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 n = 564 Health Status: unhealthy Condition: Axillary Hyperhidrosis Age Group: Mean age 33 years Sex: M+F Population Size: 564 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 n = 564 Health Status: unhealthy Condition: Axillary Hyperhidrosis Age Group: Mean age 33 years Sex: M+F Population Size: 564 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 n = 31 Health Status: unhealthy Age Group: mean age 20.4 years Sex: M+F Population Size: 31 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 n = 31 Health Status: unhealthy Age Group: mean age 20.4 years Sex: M+F Population Size: 31 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 n = 31 Health Status: unhealthy Age Group: mean age 20.4 years Sex: M+F Population Size: 31 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 n = 31 Health Status: unhealthy Age Group: mean age 20.4 years Sex: M+F Population Size: 31 Sources: |
Xerostomia | 12.5% Disc. AE |
2 mg 2 times / day multiple, oral (typical) Studied dose Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: |
unhealthy, mean age 33 years n = 24 Health Status: unhealthy Condition: hyperhidrosis Age Group: mean age 33 years Sex: M+F Population Size: 24 Sources: |
Erectile dysfunction | 4.2% Disc. AE |
2 mg 2 times / day multiple, oral (typical) Studied dose Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: |
unhealthy, mean age 33 years n = 24 Health Status: unhealthy Condition: hyperhidrosis Age Group: mean age 33 years Sex: M+F Population Size: 24 Sources: |
Headaches | 4.2% Disc. AE |
2 mg 2 times / day multiple, oral (typical) Studied dose Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: |
unhealthy, mean age 33 years n = 24 Health Status: unhealthy Condition: hyperhidrosis Age Group: mean age 33 years Sex: M+F Population Size: 24 Sources: |
Urinary retention | 4.2% Disc. AE |
2 mg 2 times / day multiple, oral (typical) Studied dose Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: |
unhealthy, mean age 33 years n = 24 Health Status: unhealthy Condition: hyperhidrosis Age Group: mean age 33 years Sex: M+F Population Size: 24 Sources: |
Dry mouth | 50% | 2 mg 2 times / day multiple, oral (typical) Studied dose Dose: 2 mg, 2 times / day Route: oral Route: multiple Dose: 2 mg, 2 times / day Sources: |
unhealthy, mean age 33 years n = 24 Health Status: unhealthy Condition: hyperhidrosis Age Group: mean age 33 years Sex: M+F Population Size: 24 Sources: |
Nocturia | grade 1, 11.1% | 3 mg 3 times / day multiple, oral (max) Studied dose Dose: 3 mg, 3 times / day Route: oral Route: multiple Dose: 3 mg, 3 times / day Sources: |
healthy, mean age 44 years n = 18 Health Status: healthy Age Group: mean age 44 years Sex: M+F Population Size: 18 Sources: |
Dry mouth | grade 1, 16.7% | 3 mg 3 times / day multiple, oral (max) Studied dose Dose: 3 mg, 3 times / day Route: oral Route: multiple Dose: 3 mg, 3 times / day Sources: |
healthy, mean age 44 years n = 18 Health Status: healthy Age Group: mean age 44 years Sex: M+F Population Size: 18 Sources: |
Chest pain | grade 1, 5.6% | 3 mg 3 times / day multiple, oral (max) Studied dose Dose: 3 mg, 3 times / day Route: oral Route: multiple Dose: 3 mg, 3 times / day Sources: |
healthy, mean age 44 years n = 18 Health Status: healthy Age Group: mean age 44 years Sex: M+F Population Size: 18 Sources: |
Headache | grade 1, 5.6% | 3 mg 3 times / day multiple, oral (max) Studied dose Dose: 3 mg, 3 times / day Route: oral Route: multiple Dose: 3 mg, 3 times / day Sources: |
healthy, mean age 44 years n = 18 Health Status: healthy Age Group: mean age 44 years Sex: M+F Population Size: 18 Sources: |
Hypoesthesia | grade 1, 5.6% | 3 mg 3 times / day multiple, oral (max) Studied dose Dose: 3 mg, 3 times / day Route: oral Route: multiple Dose: 3 mg, 3 times / day Sources: |
healthy, mean age 44 years n = 18 Health Status: healthy Age Group: mean age 44 years Sex: M+F Population Size: 18 Sources: |
Nasal dryness | grade 1, 5.6% | 3 mg 3 times / day multiple, oral (max) Studied dose Dose: 3 mg, 3 times / day Route: oral Route: multiple Dose: 3 mg, 3 times / day Sources: |
healthy, mean age 44 years n = 18 Health Status: healthy Age Group: mean age 44 years Sex: M+F Population Size: 18 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 n = 459 Health Status: unhealthy Condition: Axillary Hyperhidrosis Age Group: median age 31 years Sex: M+F Population Size: 459 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 n = 459 Health Status: unhealthy Condition: Axillary Hyperhidrosis Age Group: median age 31 years Sex: M+F Population Size: 459 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 n = 459 Health Status: unhealthy Condition: Axillary Hyperhidrosis Age Group: median age 31 years Sex: M+F Population Size: 459 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 n = 459 Health Status: unhealthy Condition: Axillary Hyperhidrosis Age Group: median age 31 years Sex: M+F Population Size: 459 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 n = 1 Health Status: unhealthy Condition: Axillary Hyperhidrosis Population Size: 1 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 n = 1 Health Status: unhealthy Condition: Axillary Hyperhidrosis Population Size: 1 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 n = 1 Health Status: unhealthy Condition: Axillary Hyperhidrosis Population Size: 1 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 n = 1 Health Status: unhealthy Condition: Axillary Hyperhidrosis Population Size: 1 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 n = 1 Health Status: unhealthy Condition: Axillary Hyperhidrosis Population Size: 1 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 n = 1 Health Status: unhealthy Condition: Axillary Hyperhidrosis Population Size: 1 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 n = 1 Health Status: unhealthy Condition: Axillary Hyperhidrosis Population Size: 1 Sources: |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
OverviewOther
Other Inhibitor | Other Substrate | Other Inducer |
---|---|---|
Drug as perpetrator
Drug as victim
PubMed
Title | Date | PubMed |
---|---|---|
Comparative study of atropine and glycopyrrolate on suxamethonium-induced changes in cardiac rate and rhythm. | 1980 Mar |
|
Effects of oral potassium supplements on upper gastrointestinal mucosa: multicenter clinical comparison of three formulations and placebo. | 1986 |
|
Twelve-hour bronchodilation in asthma with a single aerosol dose of the anticholinergic compound glycopyrrolate. | 1988 Jul |
|
[A comparison of the two anticholinergic agents atropine and glycopyrrolate during antagonism of a muscle relaxation with pyridostigmine]. | 1993 |
|
Attenuation of vagal reflexes during tracheal intubation following vagotonic anesthetic agents. | 1994 Oct |
|
Asystole associated with iohexol myelography in a dog. | 1997 Jul-Aug |
|
Postoperative reparalysis after rocuronium following nebulized epinephrine. | 1997 Mar |
|
Neuromuscular blockade after clindamycin administration: a case report. | 1999 May |
|
Treatment of compensatory gustatory hyperhidrosis with topical glycopyrrolate. | 2003 Aug 30 |
|
Pharmacokinetic and pharmacodynamic evaluations of the zwitterionic metabolite of a new series of N-substituted soft anticholinergics. | 2005 Dec |
|
Urinary retention caused by topical glycopyrrolate for hyperhidrosis. | 2006 Sep |
|
The discovery of new spirocyclic muscarinic M3 antagonists. | 2010 Dec 15 |
|
Topical glycopyrrolate reduces axillary hyperhidrosis. | 2016 Dec |
|
Role of nebulized glycopyrrolate in the treatment of chronic obstructive pulmonary disease. | 2017 |
|
Glycopyrrolate: It's time to review. | 2017 Feb |
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 |
Chemical
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