Pilocarpine Hcl (pilocarpine HCl)
Systemic Xerostomia Agents Oral Tablet
Last reviewed · Source: First Databank (FDB) drug data
Overview
Pilocarpine hydrochloride is a cholinergic agonist that binds to muscarinic receptors.
Pilocarpine hydrochloride, an alkaloid imidazole, is a cholinergic agonist that exerts a broad spectrum of pharmacologic effects with predominant muscarinic action. In sufficient dosages, muscarinic agonists can increase exocrine (e.g., salivary, sweat) gland secretion. Pilocarpine also may increase bronchial smooth muscle tone and enhance tone and motility of GI, urinary tract, gallbladder, and biliary duct smooth muscle.
A paradoxical effect of pilocarpine on the cardiovascular system has been observed; the expected effect is vasodepression, but pilocarpine may produce hypertension after a brief episode of hypotension.
Pilocarpine is pharmacologically similar to cevimeline, another oral cholinergic agonist. Both drugs stimulate residual salivary gland tissues and have been shown to substantially increase salivary flow. However, the adverse effect profile of the drugs may differ based on differences in selectivity and affinity for specific muscarinic receptor subtypes.
Cevimeline is a more selective muscarinic agonist than pilocarpine and exhibits a 40-fold greater affinity for M3 muscarinic receptors in the lacrimal and salivary glands than for M2 receptors in cardiac tissue.
In a study in healthy individuals, the onset of effect of pilocarpine was 20 minutes; maximum effect occurred at 1 hour and duration of effect was 3-5 hours. There is limited information regarding the metabolism and excretion of pilocarpine. Inactivation of the drug is thought to occur at neuronal synapses and possibly also in plasma.
Inactive or minimally active degradation products are excreted in urine.
USES: This medication is used to treat symptoms of dry mouth due to a certain immune disease (Sjogren's syndrome) or from saliva gland damage due to radiation treatments of the head/neck for cancer. Pilocarpine belongs to a class of drugs known as cholinergic agonists. It works by stimulating certain nerves to increase the amount of saliva you produce, making it easier and more comfortable to speak and swallow.
Generic name: pilocarpine HCl
Pronunciation: (PYE-loe-KAR-peen)
Drug class: Systemic Xerostomia Agents
Therapeutic class: Mouth-Throat-Dental - Preparations
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
Today’s intelligence on Pilocarpine Hcl
Indications
The following indications are listed for Pilocarpine Hcl:
- Xerostomia
- Xerostomia Secondary To Radiation Therapy
- Xerostomia Secondary To Sjogren's Syndrome
Also known as: Mouth Dryness, Mouth Dryness Secondary To Radiation Therapy, Xerostomia Secondary To Gougerot-Sjogren Disease, Xerostomia Secondary To Sicca Syndrome, Xerostomia Secondary To Sjogren's Disease.
Dosing
No dosing information is available for this tab.
Pilocarpine hydrochloride is administered orally 3 or 4 times daily.
Although food may decrease the rate of absorption, the manufacturers make no specific recommendations for administering the drug with regard to meals.
| Drug label | Dosing type | Instructions |
|---|---|---|
| Pilocarpine Hcl 5 Mg Tablet | Maintenance | Take 1 tablet (5 mg) by oral route 3 times per day. |
| Pilocarpine Hcl 7.5 Mg Tablet | Maintenance | Take 1 tablet (7.5 mg) by oral route 2 times per day. |
| Drug label | Dosing type | Instructions |
|---|---|---|
| Pilocarpine Hcl 5 Mg Tablet | Maintenance | Take 1 tablet (5 mg) by oral route 3 times per day. |
| Pilocarpine Hcl 7.5 Mg Tablet | Maintenance | Take 1 tablet (7.5 mg) by oral route 2 times per day. |
Drug interactions
There is no enhanced messaging for this drug.
There are no contraindication interactions for this drug.
There are no severe interactions for this drug.
Moderate Interaction: Assess the risk to the patient and take action as needed.
Cholinergics/Quinidine
SEVERITY LEVEL: 3-Moderate Interaction: Assess the risk to the patient and take action as needed.
MECHANISM OF ACTION: The anticholinergic properties of quinidine may oppose cholinergic drug effects.
CLINICAL EFFECTS: Quinidine may antagonize the effects of cholinergic drugs in the treatment of myasthenia gravis. Cardiac slowing secondary to cholinergic drugs would tend to be prevented by quinidine.
PREDISPOSING FACTORS: None determined.
PATIENT MANAGEMENT: If both drugs are administered, observe the myasthenic patient for signs and symptoms of the disease.
DISCUSSION: Caution is warranted in co-administration of these drugs due to their opposing pharmacologic properties.
Contraindications
Known hypersensitivity to pilocarpine hydrochloride, uncontrolled asthma, and when miosis is undesirable (e.g., acute iritis, angle-closure glaucoma).
- Angle-closure glaucoma
- Iritis
- Severe persistent asthma
- Biliary calculus
- Biliary tract disorder
- Cholecystitis
- Chronic obstructive pulmonary disease
- Disease of liver
- Psychotic disorder
- Retinal detachment
- Hypertension
- Hypotension
- Kidney stone
Adverse reactions
Adverse effects occurring in 5% or more of patients receiving pilocarpine for radiation-induced dry mouth include sweating, nausea, rhinitis, diarrhea, chills, flushing, urinary frequency, dizziness, asthenia, headache, dyspepsia, lacrimation, and edema.
Adverse effects occurring in 5% or more of patients receiving pilocarpine for dry mouth secondary to Sjogren syndrome include sweating, urinary frequency, nausea, flushing, rhinitis, diarrhea, headache, flu syndrome, dyspepsia, and dizziness.
Rare or Very Rare
- Abnormal ECG
- Bradycardia
- Hearing loss
More Frequent
- Chills
- Diarrhea
- Dizziness
- Flushing
- General weakness
- Hyperhidrosis
- Increased urinary frequency
- Nausea
- Rhinitis
Less Frequent
- Acute abdominal pain
- Dyspepsia
- Edema
- Eye tearing
- Headache disorder
- Hypertension
- Pharyngitis
- Toxic amblyopia
- Vomiting
Rare or Very Rare
- Abnormal vaginal bleeding
- Acute cognitive impairment
- Appetite changes
- Body odor
- Dysphagia
- Dysuria
- Epistaxis
- Esophagitis
- Fatigue
- Hypothermia
- Muscle fasciculation
- Palpitations
- Paresthesia
- Symptoms of anxiety
- Syncope
- Tachycardia
- Tremor
- Visual changes
- Voice change
Precautions
No enhanced messaging available.
Safety and efficacy of pilocarpine have not been established in children.
There are no adequate and well-controlled studies of pilocarpine in pregnant women; skeletal malformations, reduced fetal body weight, stillbirths, and decreased neonatal survival have been observed in animal reproductive studies at pilocarpine hydrochloride dosages higher than the maximum recommended dosages in humans.
Pilocarpine should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
It is not known whether pilocarpine is distributed into human milk. Because many drugs are distributed into human milk, a decision should be made whether to discontinue nursing or the drug, taking into account the importance of the drug to the woman.
In clinical studies in patients with head and neck cancer, adverse effects of pilocarpine in geriatric patients older than 65 years of age generally were similar to those observed in younger adults.
In clinical studies in patients with Sjogren syndrome, adverse effects of pilocarpine in geriatric patients older than 65 years of age generally were similar to those observed in younger individuals; however, urinary frequency, diarrhea, and dizziness occurred at higher rates in geriatric patients.
ICD codes
| Code | Type | Description |
|---|---|---|
| Xerostomia | ||
| K11.7 | ICD10CM | Disturbances of salivary secretion |
| R68.2 | ICD10CM | Dry mouth, unspecified |
| Xerostomia secondary to radiation therapy | ||
| K11.7 | ICD10CM | Disturbances of salivary secretion |
| R68.2 | ICD10CM | Dry mouth, unspecified |
| Xerostomia secondary to sjogren's syndrome | ||
| M35.00 | ICD10CM | Sjogren syndrome, unspecified |
| M35.0C | ICD10CM | Sjogren syndrome with dental involvement |
ICD code information from First Databank (FDB).
Formulary status
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Last reviewed · Source: First Databank (FDB) drug data
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