Reserpine (Serpasil) - Uses, Dose, Side effects, Brands

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

Risk Factor C (Monitor therapy)

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

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