Reserpine reduces blood pressure via depletion of sympathetic biogenic amines (norepinephrine and dopamine).
Reserpine (Serpasil) Uses:
-
Agitated psychotic states:
-
It is used in the treatment of agitated psychotic states (schizophrenia)
-
-
Hypertension:
-
It is used in the treatment of mild to moderate hypertension.
-
It is not recommended for the initial treatment of hypertension.
-
Reserpine (Serpasil) Dose in Adults:
- Reserpine tablets are no longer available in the US.
Reserpine (Serpasil) Dosage as an alternative agent in the treatment of Hypertension:
- The initial dose is 0.1 mg once daily
- Then titrate as needed based on patient response up to 0.25 mg once daily
- Clinically, the need for a "loading" period (as recommended by the manufacturer) is not supported well, and the above dosing is preferred.
Reserpine (Serpasil) Dosage in the treatment of Schizophrenia:
- Dosing recommendations usually vary
- initial dose recommendations range from 0.05 to 0.25 mg.
- It may be increased in increments of 0.1 to 0.25 mg
Reserpine (Serpasil) Dose in Children
The safety and efficacy of reserpine in children is not established.
Reserpine pregnancy Risk Factor C
- It can also cross the placenta.
- In animal reproduction studies using parenteral administration, teratogenic events were observed.
- The non-teratogenic effects of reserpine on newborns could include anorexia and cyanosis as well as increased secretions in the respiratory tract.
Use while breastfeeding
- It can be found in breast milk
- Breastfed infants have experienced anorexia and cyanosis, as well as increased secretions of their respiratory tract.
Reserpine (Serpasil) dose in Renal disease:
- The manufacturer's label does not include any dosage adjustments.
- Some experts have used the following dosing adjustments:
-
CrCl 10mL/minute
- Avoid excessive usage
-
Peritoneal dialysis and hemoodialysis
- Hemo- or peritoneal dialysis cannot remove it
- Supplemental dosages are not required.
Serpasil dose in liver disease:
- No dosage adjustment is given in the manufacturer’s labeling.
Side effects of Reserpine (Serpasil):
-
Cardiovascular:
- Bradycardia
- Cardiac Arrhythmia
- Chest Pain
- Flushing
- Hypotension
- Peripheral Edema
- Syncope
- Ventricular Premature Contractions
-
Central Nervous System:
- Anxiety (Paradoxical)
- Decreased Mental Acuity
- Depression
- Dizziness
- Drowsiness
- Drug-Induced Parkinson’s Disease
- Fatigue
- Headache
- Nightmares
- Nervousness
-
Dermatologic:
- Pruritus
- Skin Rash
-
Endocrine & Metabolic:
- Gynecomastia
- Decreased Libido
- Weight Gain
-
Gastrointestinal:
- Anorexia
- Diarrhea
- Hyperacidity
- Nausea
- Sialorrhea
- Vomiting
- Xerostomia
-
Genitourinary:
- Impotence
-
Hematologic & Oncologic:
- Immune Thrombocytopenia
- Purpura
-
Neuromuscular & Skeletal:
- Myalgia
-
Ophthalmic:
- Blurred Vision
- Optic Atrophy
-
Respiratory:
- Dyspnea
- Epistaxis
- Nasal Congestion
Contraindication to Reserpine (Serpasil):
- Hypersensitivity to any component of the drug/preparation
- Active peptic ulcer disease, and ulcerative colitis
- History of mental depression, especially with suicidal tendencies
- Patients who have received electroconvulsive treatment (ECT)
Warnings and precautions
-
CNS effects
- High doses can cause severe mental depression, anxiety, and psychosis (uncommon with dosages below 0.25 mg/day).
-
Orthostatic hypotension
- It can lead to orthostatic hypotension
- Use caution in patients at high risk of hypotension, or patients with transient hypotensive episodes that are difficult to tolerate (cardiovascular disease and cerebrovascular disease).
-
Asthma
- Use caution in patients suffering from asthma.
-
Gallstones
- Patients with gallstones should be treated with caution
-
Gastrointestinal Disease:
- Patients with inflammatory bowel disease and a history of peptic ulcer disease should be cautious.
-
Parkinson disease
- Patients with Parkinson's disease should be treated with caution
-
Renal impairment
- Patients with impaired renal function should be cautious.
Reserpine (United States: Not available): Drug Interaction
Acebrophylline |
May enhance the tachycardic effect of Reserpine. |
Alcohol (Ethyl) |
CNS Depressants may enhance the CNS depressant effect of Alcohol (Ethyl). |
Alfuzosin |
May enhance the hypotensive effect of Blood Pressure Lowering Agents. |
Alizapride |
May enhance the CNS depressant effect of CNS Depressants. |
Amezinium |
May enhance the adverse/toxic effect of Reserpine. |
Amphetamines |
Gastrointestinal Acidifying Agents may decrease the serum concentration of Amphetamines. |
Amphetamines |
May diminish the antihypertensive effect of Antihypertensive Agents. |
Antipsychotic Agents (Second Generation [Atypical]) |
Blood Pressure Lowering Agents may enhance the hypotensive effect of Antipsychotic Agents (Second Generation [Atypical]). |
Barbiturates |
May enhance the hypotensive effect of Blood Pressure Lowering Agents. |
Benperidol |
May enhance the hypotensive effect of Blood Pressure Lowering Agents. |
Beta-Blockers |
Reserpine may enhance the hypotensive effect of Beta-Blockers. |
Brexanolone |
CNS Depressants may enhance the CNS depressant effect of Brexanolone. |
Brigatinib |
May diminish the antihypertensive effect of Antihypertensive Agents. Brigatinib may enhance the bradycardic effect of Antihypertensive Agents. |
Brimonidine (Topical) |
May enhance the CNS depressant effect of CNS Depressants. |
Brimonidine (Topical) |
May enhance the hypotensive effect of Blood Pressure Lowering Agents. |
Bromopride |
May enhance the CNS depressant effect of CNS Depressants. |
Cannabidiol |
May enhance the CNS depressant effect of CNS Depressants. |
Cannabis |
May enhance the CNS depressant effect of CNS Depressants. |
Cardiac Glycosides |
Reserpine may enhance the adverse/toxic effect of Cardiac Glycosides. |
Chlorphenesin Carbamate |
May enhance the adverse/toxic effect of CNS Depressants. |
CNS Depressants |
May enhance the adverse/toxic effect of other CNS Depressants. |
Dexmethylphenidate |
May diminish the therapeutic effect of Antihypertensive Agents. |
Diazoxide |
May enhance the hypotensive effect of Blood Pressure Lowering Agents. |
Dimethindene (Topical) |
May enhance the CNS depressant effect of CNS Depressants. |
Doxylamine |
May enhance the CNS depressant effect of CNS Depressants. Management: The manufacturer of Diclegis (doxylamine/pyridoxine), intended for use in pregnancy, specifically states that use with other CNS depressants is not recommended. |
Dronabinol |
May enhance the CNS depressant effect of CNS Depressants. |
DULoxetine |
Blood Pressure Lowering Agents may enhance the hypotensive effect of DULoxetine. |
Esketamine |
May enhance the CNS depressant effect of CNS Depressants. |
Herbs (Hypertensive Properties) |
May diminish the antihypertensive effect of Antihypertensive Agents. |
Herbs (Hypotensive Properties) |
May enhance the hypotensive effect of Blood Pressure Lowering Agents. |
HydrOXYzine |
May enhance the CNS depressant effect of CNS Depressants. |
Hypotension-Associated Agents |
Blood Pressure Lowering Agents may enhance the hypotensive effect of Hypotension-Associated Agents. |
Kava Kava |
May enhance the adverse/toxic effect of CNS Depressants. |
Levodopa-Containing Products |
Blood Pressure Lowering Agents may enhance the hypotensive effect of Levodopa-Containing Products. |
Lofexidine |
May enhance the CNS depressant effect of CNS Depressants. Management: Drugs listed as exceptions to this monograph are discussed in further detail in separate drug interaction monographs. |
Lormetazepam |
May enhance the hypotensive effect of Blood Pressure Lowering Agents. |
Magnesium Sulfate |
May enhance the CNS depressant effect of CNS Depressants. |
Methylphenidate |
May diminish the antihypertensive effect of Antihypertensive Agents. |
MetyroSINE |
CNS Depressants may enhance the sedative effect of MetyroSINE. |
Minocycline |
May enhance the CNS depressant effect of CNS Depressants. |
Mirtazapine |
CNS Depressants may enhance the CNS depressant effect of Mirtazapine. |
Molsidomine |
May enhance the hypotensive effect of Blood Pressure Lowering Agents. |
Nabilone |
May enhance the CNS depressant effect of CNS Depressants. |
Naftopidil |
May enhance the hypotensive effect of Blood Pressure Lowering Agents. |
Nicergoline |
May enhance the hypotensive effect of Blood Pressure Lowering Agents. |
Nicorandil |
May enhance the hypotensive effect of Blood Pressure Lowering Agents. |
Nitroprusside |
Blood Pressure Lowering Agents may enhance the hypotensive effect of Nitroprusside. |
Pentoxifylline |
May enhance the hypotensive effect of Blood Pressure Lowering Agents. |
Pholcodine |
Blood Pressure Lowering Agents may enhance the hypotensive effect of Pholcodine. |
Phosphodiesterase 5 Inhibitors |
May enhance the hypotensive effect of Blood Pressure Lowering Agents. |
Piribedil |
CNS Depressants may enhance the CNS depressant effect of Piribedil. |
Pizotifen |
May diminish the antihypertensive effect of Reserpine. |
Pramipexole |
CNS Depressants may enhance the sedative effect of Pramipexole. |
Prostacyclin Analogues |
May enhance the hypotensive effect of Blood Pressure Lowering Agents. |
Quinagolide |
May enhance the hypotensive effect of Blood Pressure Lowering Agents. |
QuiNIDine |
Reserpine may enhance the adverse/toxic effect of QuiNIDine. |
ROPINIRole |
CNS Depressants may enhance the sedative effect of ROPINIRole. |
Rotigotine |
CNS Depressants may enhance the sedative effect of Rotigotine. |
Rufinamide |
May enhance the adverse/toxic effect of CNS Depressants. Specifically, sleepiness and dizziness may be enhanced. |
Selective Serotonin Reuptake Inhibitors |
CNS Depressants may enhance the adverse/toxic effect of Selective Serotonin Reuptake Inhibitors. Specifically, the risk of psychomotor impairment may be enhanced. |
Tetrahydrocannabinol |
May enhance the CNS depressant effect of CNS Depressants. |
Tetrahydrocannabinol and Cannabidiol |
May enhance the CNS depressant effect of CNS Depressants. |
Trimeprazine |
May enhance the CNS depressant effect of CNS Depressants. |
Yohimbine |
May diminish the antihypertensive effect of Antihypertensive Agents. |
Risk Factor D (Consider therapy modification) |
|
Amifostine |
Blood Pressure Lowering Agents may enhance the hypotensive effect of Amifostine. Management: When amifostine is used at chemotherapy doses, blood pressure lowering medications should be withheld for 24 hours prior to amifostine administration. If blood pressure lowering therapy cannot be withheld, amifostine should not be administered. |
Blonanserin |
CNS Depressants may enhance the CNS depressant effect of Blonanserin. |
Buprenorphine |
CNS Depressants may enhance the CNS depressant effect of Buprenorphine. Management: Consider reduced doses of other CNS depressants, and avoiding such drugs in patients at high risk of buprenorphine overuse/self-injection. Initiate buprenorphine at lower doses in patients already receiving CNS depressants. |
Chlormethiazole |
May enhance the CNS depressant effect of CNS Depressants. Management: Monitor closely for evidence of excessive CNS depression. The chlormethiazole labeling states that an appropriately reduced dose should be used if such a combination must be used. |
Cladribine |
Inhibitors of Equilibrative Nucleoside (ENT1) and Concentrative Nucleoside (CNT3) Transport Proteins may increase the serum concentration of Cladribine. Management: Avoid concomitant use of ENT1 or CNT3 inhibitors during the 4 to 5 day oral cladribine treatment cycles whenever possible. If combined, consider an ENT1 or CNT3 inhibitor dose reduction and separation in the timing of administration. |
Droperidol |
May enhance the CNS depressant effect of CNS Depressants. Management: Consider dose reductions of droperidol or of other CNS agents (eg, opioids, barbiturates) with concomitant use. Exceptions to this monograph are discussed in further detail in separate drug interaction monographs. |
Flunitrazepam |
CNS Depressants may enhance the CNS depressant effect of Flunitrazepam. |
HYDROcodone |
CNS Depressants may enhance the CNS depressant effect of HYDROcodone. Management: Avoid concomitant use of hydrocodone and benzodiazepines or other CNS depressants when possible. These agents should only be combined if alternative treatment options are inadequate. If combined, limit the dosages and duration of each drug. |
Methotrimeprazine |
CNS Depressants may enhance the CNS depressant effect of Methotrimeprazine. Methotrimeprazine may enhance the CNS depressant effect of CNS Depressants. Management: Reduce adult dose of CNS depressant agents by 50% with initiation of concomitant methotrimeprazine therapy. Further CNS depressant dosage adjustments should be initiated only after clinically effective methotrimeprazine dose is established. |
Monoamine Oxidase Inhibitors |
May enhance the adverse/toxic effect of Reserpine. Existing MAOI therapy can result in paradoxical effects of added reserpine (e.g., excitation, hypertension). Management: Monoamine oxidase inhibitors (MAOIs) should be avoided or used with great caution in patients who are also receiving reserpine. |
Obinutuzumab |
May enhance the hypotensive effect of Blood Pressure Lowering Agents. Management: Consider temporarily withholding blood pressure lowering medications beginning 12 hours prior to obinutuzumab infusion and continuing until 1 hour after the end of the infusion. |
Opioid Agonists |
CNS Depressants may enhance the CNS depressant effect of Opioid Agonists. Management: Avoid concomitant use of opioid agonists and benzodiazepines or other CNS depressants when possible. These agents should only be combined if alternative treatment options are inadequate. If combined, limit the dosages and duration of each drug. |
OxyCODONE |
CNS Depressants may enhance the CNS depressant effect of OxyCODONE. Management: Avoid concomitant use of oxycodone and benzodiazepines or other CNS depressants when possible. These agents should only be combined if alternative treatment options are inadequate. If combined, limit the dosages and duration of each drug. |
Perampanel |
May enhance the CNS depressant effect of CNS Depressants. Management: Patients taking perampanel with any other drug that has CNS depressant activities should avoid complex and high-risk activities, particularly those such as driving that require alertness and coordination, until they have experience using the combination. |
Sodium Oxybate |
May enhance the CNS depressant effect of CNS Depressants. Management: Consider alternatives to combined use. When combined use is needed, consider minimizing doses of one or more drugs. Use of sodium oxybate with alcohol or sedative hypnotics is contraindicated. |
Suvorexant |
CNS Depressants may enhance the CNS depressant effect of Suvorexant. Management: Dose reduction of suvorexant and/or any other CNS depressant may be necessary. Use of suvorexant with alcohol is not recommended, and the use of suvorexant with any other drug to treat insomnia is not recommended. |
Tapentadol |
May enhance the CNS depressant effect of CNS Depressants. Management: Avoid concomitant use of tapentadol and benzodiazepines or other CNS depressants when possible. These agents should only be combined if alternative treatment options are inadequate. If combined, limit the dosages and duration of each drug. |
Zolpidem |
CNS Depressants may enhance the CNS depressant effect of Zolpidem. Management: Reduce the Intermezzo brand sublingual zolpidem adult dose to 1.75 mg for men who are also receiving other CNS depressants. No such dose change is recommended for women. Avoid use with other CNS depressants at bedtime; avoid use with alcohol. |
Risk Factor X (Avoid combination) |
|
Azelastine (Nasal) |
CNS Depressants may enhance the CNS depressant effect of Azelastine (Nasal). |
Bromperidol |
Blood Pressure Lowering Agents may enhance the hypotensive effect of Bromperidol. Bromperidol may diminish the hypotensive effect of Blood Pressure Lowering Agents. |
Bromperidol |
May enhance the CNS depressant effect of CNS Depressants. |
Deutetrabenazine |
Reserpine may enhance the adverse/toxic effect of Deutetrabenazine. |
Iobenguane Radiopharmaceutical Products |
Reserpine may diminish the therapeutic effect of Iobenguane Radiopharmaceutical Products. Management: Discontinue all drugs that may inhibit or interfere with catecholamine transport or uptake for at least 5 biological half-lives before iobenguane administration. Do not administer reserpine until at least 7 days after each iobenguane dose. |
Orphenadrine |
CNS Depressants may enhance the CNS depressant effect of Orphenadrine. |
Oxomemazine |
May enhance the CNS depressant effect of CNS Depressants. |
Paraldehyde |
CNS Depressants may enhance the CNS depressant effect of Paraldehyde. |
Tetrabenazine |
Reserpine may enhance the adverse/toxic effect of Tetrabenazine. |
Thalidomide |
CNS Depressants may enhance the CNS depressant effect of Thalidomide. |
Monitor:
- Blood pressure, standing and sitting/supine
How to administer Reserpine?
- It may be administered with or without meals orally.
Mechanism of action of Reserpine (Serpasil):
- It lowers blood pressure by depleting sympathetic biogenic amines (norepinephrine, dopamine).
- Sedative effects are also common.
Onset of action:
- Antihypertensive effect: 3-6 days
Duration:
- 2-6 weeks
Absorption:
- almost 40%
Protein binding:
- 96%
Metabolism:
- mainly hepatic (>90%)
Half-life elimination:
- 50-100 hours
Excretion:
- From Feces (30% to 60%) & urine (10%)
International Brands of Reserpine:
- Raupasil
- Rauserpine
- Rauverid
- Reselpin
- Respine
- Serpalan
- Serpasil
Reserpine (Serpasil) Brand Names in Pakistan:
Reserpine Tablets 0.25 mg |
|
Reserpine | Specific Research Laboratories |