Nimodipine is a medication primarily used for the treatment of subarachnoid hemorrhage (SAH), a type of bleeding in the space around the brain. It belongs to a class of medications called calcium channel blockers. Nimodipine works by relaxing blood vessels in the brain, which helps to prevent or reduce the severity of brain damage caused by reduced blood flow in cases of SAH. It is usually administered orally or via a feeding tube, as it comes in the form of capsules or oral solution.
Nimodipine (Nimotop) is a calcium channel blocker that improves neurological outcomes in patients with subarachnoid hemorrhage (ruptured berry aneurysm).
Nimodipine Uses (indications):
- Subarachnoid hemorrhage:
- It is used for the improvement of neurological outcome by reducing in adult patients the incidence & severity of ischemic deficits with subarachnoid hemorrhage (SAH) from ruptured intracranial berry aneurysms regardless of their post ictus neurological condition (ie, Hunt and Hess grades I to V)
Nimodipine (Nimotop) Dose in Adults
Note:
- Nimodipine is a medicine that you take by mouth.
Nimodipine (Nimotop) Dose in the treatment of Subarachnoid hemorrhage:
- The typical dose is 60 milligrams, and you take it every 4 hours for 21 days straight.
- It's essential to start taking it within 96 hours of when the brain bleeding started.
Use in Children:
Not indicated
Pregnancy Risk Category: C
- Nimodipine is a medication that can pass from a pregnant person to their baby.
- It's been looked at for treating a condition called preeclampsia, which involves high blood pressure during pregnancy.
- However, it's not one of the drugs recommended for treating severe high blood pressure during labor or after giving birth due to preeclampsia or eclampsia.
Use of Nimodipine while breastfeeding
- Nimodipine can be found in breast milk, but in very small amounts.
- Studies have shown that the amount of nimodipine a baby might get through breast milk is less than 1% of the mother's dose, which is considered safe for breastfeeding according to general guidelines.
- One study looked at a mother who took oral nimodipine for 10 days after giving birth, and another studied a mother who received nimodipine through an IV infusion.
- In both cases, the amount of nimodipine in breast milk was low and varied, but it was related to the amount in the mother's blood.
- However, because there's a possibility of serious side effects in breastfed babies, the manufacturer suggests considering whether to continue breastfeeding or stop taking the medication, weighing the benefits of treatment for the mother against the potential risks to the baby.
Nimodipine (Nimotop) Dose in Kidney Disease:
- The manufacturer's instructions for nimodipine do not include any specific adjustments for dosage based on kidney function.
- This is because nimodipine is mostly removed from the body through processes other than the kidneys, so changes in kidney function are not expected to significantly affect its elimination.
- Additionally, nimodipine is not removed by dialysis, so there's no need for an extra dose after dialysis.
Dose in Liver disease:
- In patients with hepatic impairment, specifically cirrhosis, it's often necessary to adjust medication dosages due to changes in how the liver processes drugs.
- For nimodipine, a reduced dosage of 30 milligrams every 4 hours is recommended for these patients to ensure safety and effectiveness.
Side Effects of Nimodipine (Nimotop):
- Cardiovascular:
- Decreased blood pressure
- Bradycardia
- Central nervous system:
- Headache
- Gastrointestinal:
- Nausea
Contraindication to Nimodipine (Nimotop):
- In the United States, the labeling for nimodipine advises against its use with strong inhibitors of the enzyme CYP3A4, which include medications like clarithromycin, ketoconazole, and ritonavir, among others.
- However, there are no contraindications listed in the manufacturer's labeling for Nymalize, a formulation of nimodipine.
- In Canada, nimodipine should not be used in individuals who have a known hypersensitivity to nimodipine or any of the components in its formulation. Additionally, concomitant use with certain medications like phenobarbital, phenytoin, carbamazepine, or rifampin is not recommended.
Warnings and precautions
Angina/MI
- When starting or adjusting the dosage of dihydropyridine calcium channel blockers, like nimodipine, there's a risk of increased angina (chest pain) or myocardial infarction (heart attack).
- This is because these medications can lead to reflex tachycardia, a rapid heart rate, which might worsen angina or trigger a heart attack in patients with obstructive coronary disease, particularly if they are not concurrently taking beta-blockers.
Gastrointestinal events:
- During treatment with nimodipine, there have been rare reports of gastrointestinal problems like intestinal pseudo-obstruction and ileus.
- These conditions involve issues with the movement of the intestines, which can cause symptoms like bloating, constipation, and abdominal pain.
Syncope and hypotension:
- Some people may experience symptomatic hypotension, where blood pressure drops too low, while taking nimodipine, which can sometimes lead to fainting.
- It's crucial to adjust the dose of nimodipine appropriately based on the individual's condition and monitor their blood pressure closely during treatment.
- This helps ensure that blood pressure is lowered at a rate that is safe for the person.
- If any symptoms of low blood pressure or fainting occur, it's essential to seek medical attention promptly.
Peripheral edema
- Peripheral edema, swelling in the arms, legs, or other extremities, is a common side effect of nimodipine treatment.
- It typically develops within 2 to 3 weeks after starting therapy.
- While this swelling can be uncomfortable, it's generally not harmful.
Hepatic impairment
- In patients with cirrhosis, a liver condition, nimodipine should be used cautiously.
- This is because plasma concentrations of nimodipine can increase in these individuals, raising the risk of adverse reactions.
- Therefore, a lower dose of nimodipine is often needed, and it's important to closely monitor blood pressure and heart rate during treatment.
- This helps ensure the medication is safe and effective for individuals with hepatic impairment.
Hypertrophic cardiomyopathy and outflow tract obstruction
- In individuals with hypertrophic cardiomyopathy and outflow tract obstruction, caution should be exercised when using nimodipine.
- This caution is necessary because nimodipine can affect heart function, and in these patients, there may be a higher risk of complications due to the obstruction in the outflow tract of the heart.
Nimodipine: Drug Interaction
|
Risk Factor C (Monitor therapy) |
|
|
Alfuzosin |
The hypotensive effects of blood pressure-lowering medications may be strengthened. |
|
Alpha1-Blockers |
The hypotensive effects of calcium channel blockers may be strengthened. |
|
Amphetamines |
May lessen the effectiveness of antihypertensive agents. |
|
Antipsychotic Agents (Second Generation [Atypical]) |
Antipsychotic drugs' hypotensive effects may be enhanced by blood pressure-lowering medications (Second Generation [Atypical]). |
|
Aprepitant |
May elevate CYP3A4 substrates' serum concentration (High risk with Inhibitors). |
|
Atosiban |
Calcium channel blockers may intensify Atosiban's harmful or hazardous effects. Particularly, pulmonary edoema and/or dyspnea may be at higher risk. |
|
Barbiturates |
Calcium Channel Blockers' metabolic rate might be increased. Management: Keep an eye out for any diminished therapeutic effects of barbiturate medication when concurrently using calcium channel blockers. There may need to be dose modifications with calcium channel blockers. The concurrent use of phenobarbital and nimodipine is not recommended. |
|
Barbiturates |
The hypotensive effects of blood pressure-lowering medications may be strengthened. |
|
Benperidol |
The hypotensive effects of blood pressure-lowering medications may be strengthened. |
|
Bosentan |
May lower CYP3A4 substrates' serum concentration (High risk with Inhibitors). |
|
Brigatinib |
May lessen the effectiveness of antihypertensive agents. Antihypertensive Agents' bradycardic action may be strengthened by brutinib. |
|
Brimonidine (Topical) |
The hypotensive effects of blood pressure-lowering medications may be strengthened. |
|
Calcium Channel Blockers (Nondihydropyridine) |
Dihydropyridine, a calcium channel blocker, may increase the hypotensive effects of calcium channel blockers (Nondihydropyridine). Calcium Channel Blockers (Nondihydropyridine) may cause an increase in serum calcium channel blocker concentration (Dihydropyridine). |
|
Calcium Salts |
The hypotensive effects of calcium channel blockers may be strengthened. |
|
Clofazimine |
May elevate CYP3A4 substrates' serum concentration (High risk with Inhibitors). |
|
Clopidogrel |
Calcium channel blockers may reduce Clopidogrel's therapeutic efficacy. |
|
CycloSPORINE (Systemic) |
The serum concentration of CycloSPORINE may rise when Calcium Channel Blockers (Dihydropyridine) are taken (Systemic). Calcium Channel Blockers' serum levels may rise when CycloSPORINE (Systemic) is used (Dihydropyridine). |
|
CYP3A4 Inducers (Moderate) |
NiMODipine serum concentration can drop. |
|
CYP3A4 Inducers (Weak) |
NiMODipine serum concentration can drop. |
|
CYP3A4 Inhibitors (Moderate) |
NiMODipine serum concentration can drop. |
|
CYP3A4 Inhibitors (Weak) |
NiMODipine serum concentration can drop. |
|
Dapoxetine |
The orthostatic hypotensive effects of calcium channel blockers may be strengthened. |
|
Deferasirox |
May lower CYP3A4 substrates' serum concentration (High risk with Inhibitors). |
|
Diazoxide |
The hypotensive effects of blood pressure-lowering medications may be strengthened. |
|
DULoxetine |
The hypotensive impact of DULoxetine may be enhanced by blood pressure lowering medications. |
|
Duvelisib |
May elevate CYP3A4 substrates' serum concentration (High risk with Inhibitors). |
|
Efavirenz |
Calcium Channel Blockers' serum concentration can drop. |
|
Erdafitinib |
May lower CYP3A4 substrates' serum concentration (High risk with Inhibitors). |
|
Erdafitinib |
May elevate CYP3A4 substrates' serum concentration (High risk with Inhibitors). |
|
Fluconazole |
The hypotensive effects of calcium channel blockers may be strengthened. |
|
FLUoxetine |
NiMODipine serum concentration can rise. |
|
Fosaprepitant |
May elevate CYP3A4 substrates' serum concentration (High risk with Inhibitors). |
|
Fosnetupitant |
May elevate CYP3A4 substrates' serum concentration (High risk with Inhibitors). |
|
Herbs (Hypertensive Properties) |
May lessen the effectiveness of antihypertensive agents. |
|
Herbs (Hypotensive Properties) |
The hypotensive effects of blood pressure-lowering medications may be strengthened. |
|
Ivosidenib |
May lower CYP3A4 substrates' serum concentration (High risk with Inhibitors). |
|
Larotrectinib |
May elevate CYP3A4 substrates' serum concentration (High risk with Inhibitors). |
|
Levodopa-Containing Products |
Levodopa-Containing Products' hypotensive effects may be strengthened by blood pressure-lowering medications. |
|
Lormetazepam |
The hypotensive effects of blood pressure-lowering medications may be strengthened. |
|
Magnesium Salts |
Calcium channel blockers might make magnesium salts more harmful or poisonous. Calcium Channel Blockers' hypotensive effects may be strengthened by magnesium salts. |
|
Melatonin |
May reduce the effectiveness of calcium channel blockers as an antihypertensive (Dihydropyridine). |
|
Methylphenidate |
May lessen the effectiveness of antihypertensive agents. |
|
Molsidomine |
The hypotensive effects of blood pressure-lowering medications may be strengthened. |
|
Naftopidil |
The hypotensive effects of blood pressure-lowering medications may be strengthened. |
|
Netupitant |
May elevate CYP3A4 substrates' serum concentration (High risk with Inhibitors). |
|
Neuromuscular-Blocking Agents (Nondepolarizing) |
The neuromuscular-blocking impact of neuromuscular-blocking agents may be enhanced by calcium channel blockers (Nondepolarizing). |
|
Nicergoline |
The hypotensive effects of blood pressure-lowering medications may be strengthened. |
|
Nicorandil |
The hypotensive effects of blood pressure-lowering medications may be strengthened. |
|
Nitroprusside |
Nitroprusside's hypotensive impact may be strengthened by blood pressure-lowering medications. |
|
Palbociclib |
May elevate CYP3A4 substrates' serum concentration (High risk with Inhibitors). |
|
Pentoxifylline |
The hypotensive effects of blood pressure-lowering medications may be strengthened. |
|
Pholcodine |
Pholcodine's hypotensive impact may be strengthened by blood pressure lowering medications. |
|
Phosphodiesterase 5 Inhibitors |
The hypotensive effects of blood pressure-lowering medications may be strengthened. |
|
Prostacyclin Analogues |
The hypotensive effects of blood pressure-lowering medications may be strengthened. |
|
Quinagolide |
The hypotensive effects of blood pressure-lowering medications may be strengthened. |
|
QuiNIDine |
The serum concentration of QuiNIDine may be lowered by calcium channel blockers (Dihydropyridine). The serum concentration of QuiNIDine may rise in response to calcium channel blockers (Dihydropyridine). Calcium Channel Blockers' serum levels may rise in response to quinine (Dihydropyridine). |
|
Sarilumab |
May lower CYP3A4 substrates' serum concentration (High risk with Inhibitors). |
|
Siltuximab |
May lower CYP3A4 substrates' serum concentration (High risk with Inhibitors). |
|
Simeprevir |
May elevate CYP3A4 substrates' serum concentration (High risk with Inhibitors). |
|
Tacrolimus (Systemic) |
Tacrolimus serum levels may rise when Calcium Channel Blockers (Dihydropyridine) are used (Systemic). |
|
Tocilizumab |
May lower CYP3A4 substrates' serum concentration (High risk with Inhibitors). |
|
Yohimbine |
May lessen the effectiveness of antihypertensive agents. |
|
Risk Factor D (Consider therapy modification) |
|
|
Amifostine |
Amifostine's hypotensive impact may be strengthened by blood pressure lowering medications. Treatment: Blood pressure-lowering drugs need to be avoided for 24 hours before amifostine is administered when used at chemotherapeutic doses. Amifostine should not be given if blood pressure lowering treatment cannot be stopped. |
|
Cimetidine |
Calcium Channel Blockers' serum levels can rise. Management: Take cimetidine substitutes into consideration. If there is no suitable substitute, watch for increased calcium channel blocker effects after starting or increasing the dosage of cimetidine and decreased effects after stopping or decreasing the dosage. |
|
Cladribine |
The serum content of Cladribine may rise in response to inhibitors of equilibrative nucleoside (ENT1) and concentrated nucleoside (CNT3) transport proteins. Management: Whenever possible, avoid using ENT1 or CNT3 inhibitors concurrently during the 4 to 5 day oral cladribine therapy cycles. |
|
Dabrafenib |
May lower the serum level of CYP3A4 substrates (High risk with Inducers). Management: When possible, look for substitutes for the CYP3A4 substrate. If concurrent therapy cannot be avoided, pay special attention to the substrate's clinical consequences (particularly therapeutic effects). |
|
Lorlatinib |
May lower the serum level of CYP3A4 substrates (High risk with Inducers). Management: Avoid taking lorlatinib at the same time as any CYP3A4 substrates for which even a small drop in serum levels of the substrate could result in therapeutic failure and negative clinical outcomes. |
|
Macrolide Antibiotics |
Calcium Channel Blockers' metabolic rate might be decreased. Use a noninteracting macrolide as a possible management strategy. The Canadian labelling for felodipine expressly advises against using it in conjunction with clarithromycin. Azithromycin (Systemic), Fidaxomicin, Roxithromycin, and Spiramycin are exceptions. |
|
Obinutuzumab |
The hypotensive effects of blood pressure-lowering medications may be strengthened. Management: Take into account temporarily stopping blood pressure-lowering drugs 12 hours before the start of the obinutuzumab infusion and keeping them off until 1 hour after the infusion is finished. |
|
Rifamycin Derivatives |
Calcium Channel Blockers' serum concentration can drop. This predominantly affects calcium channel blockers used orally. Management: Using rifampin with certain calcium channel blockers is not advised according to the labelling in the US and Canada. Look up the relevant labelling. |
|
Sincalide |
The therapeutic benefit of Sincalide may be reduced by medications that affect gallbladder function. Prior to using sincalide to induce gallbladder contraction, you should think about stopping any medications that can impair gallbladder motility. |
|
Stiripentol |
May elevate CYP3A4 substrates' serum concentration (High risk with Inhibitors). Management: Due to the increased potential for side effects and toxicity, stiripentol should not be used with CYP3A4 substrates that are thought to have a narrow therapeutic index. Use of stiripentol with any CYP3A4 substrate necessitates closer observation. |
|
Risk Factor X (Avoid combination) |
|
|
Bromperidol |
The hypotensive impact of bromperidol may be enhanced by blood pressure lowering medications. Blood Pressure Lowering Agents' hypotensive effects may be lessened by bromperidol. |
|
Conivaptan |
May elevate CYP3A4 substrates' serum concentration (High risk with Inhibitors). |
|
CYP3A4 Inducers (Strong) |
NiMODipine serum concentration can drop. |
|
CYP3A4 Inhibitors (Strong) |
NiMODipine serum concentration can rise |
|
Fusidic Acid (Systemic) |
May elevate CYP3A4 substrates' serum concentration (High risk with Inhibitors). |
|
Grapefruit Juice |
NiMODipine serum concentration can rise |
|
Idelalisib |
May elevate CYP3A4 substrates' serum concentration (High risk with Inhibitors). |
|
St John's Wort |
NiMODipine serum concentration can drop. |
Mnitoring parameters:
- None mentioned. Monitor blood pressure the response to treatment.
- When administered to patients with subarachnoid hemorrhage, monitor for the clinical features of raised intracranial pressure.
How to administer Nimodipine (Nimotop)?
Enteral Administration Only
- Life-threatening adverse events have occurred when nimodipine is given intravenously. It must be administered through the mouth or a feeding tube.
- Administer Nimodipine on an empty stomach, at least 1 hour before or 2 hours after meals to ensure proper absorption.
Oral Administration
US Labeling
- Nimodipine should be taken on an empty stomach, at least 1 hour before or 2 hours after meals.
- Swallow the tablet whole with a glass of water; do not crush it.
- Avoid alkaline mixtures for 2 hours before or after taking nimodipine.
- Administer while sitting or standing; avoid lying down during administration.
Canadian Labeling
- Nimodipine can be taken with or without food, but it's important to take it consistently.
- Swallow the tablet whole with a glass of water; do not crush it.
- Avoid alkaline mixtures for 2 hours before or after taking nimodipine.
- Administer while sitting or standing; avoid lying down during administration.
Nasogastric (NG) or Gastric Tube Administration (Oral Solution - Nymalize)
- Administer using the supplied oral syringe labeled "ORAL USE ONLY."
- After administration, refill the oral syringe with 20 mL of normal saline and flush any remaining contents from the tube into the stomach.
Capsules
- If capsules cannot be swallowed, extract the liquid contents using an 18-gauge needle and syringe.
- Transfer the liquid contents to an oral syringe (preferably amber-colored) labeled "WARNING: For ORAL use only" or "Not for IV use."
- It's recommended to do this preparation in the pharmacy.
- Follow with a flush of 30 mL normal saline.
Mechanism of action of Nimodipine (Nimotop):
- Nimodipine belongs to the same class of medications as other calcium channel blockers.
- Animal studies suggest that nimodipine has a stronger effect on the arteries in the brain compared to those in other parts of the body.
- This increased specificity might be because nimodipine is more easily distributed in the brain and has greater fat solubility compared to other drugs like nifedipine.
- Nimodipine works by blocking calcium ions from entering specific areas of smooth muscle cells in blood vessels and the heart during periods of electrical stimulation.
- This action helps relax and widen blood vessels, which can improve blood flow, particularly in the brain.
Protein Binding:
- Nimodipine binds to proteins in the blood at a rate of over 95%, which means most of it is attached to proteins and less is available to act in the body.
Metabolism:
- Nimodipine is mainly broken down by the liver through a process involving the enzyme CYP3A4. This breakdown happens primarily in the liver before the drug reaches the bloodstream.
Bioavailability:
- The amount of nimodipine that actually gets into the bloodstream varies depending on the form it's taken in.
- In capsule form, around 13% of the drug is absorbed, while in tablet form (specifically in the Canadian product), it's about 16%. However, this can range from 3% to 30% in different individuals.
Half-life Elimination:
- Nimodipine typically stays in the body for 1 to 2 hours before it's eliminated. This time can be longer in people with kidney problems, as the drug is cleared from the body more slowly.
Time to Peak, Serum:
- After taking nimodipine, it reaches its highest concentration in the blood, known as peak serum level, in about 1 hour.
Excretion:
- Nimodipine is primarily eliminated from the body through urine, with less than 1% being excreted unchanged. A small portion may also be eliminated in feces.
International Brands of Nimodipine:
- Nimodipine
- Nimotop
- Amocure
- Brainal
- Eftipine
- Eugerial
- Grifonimod
- Irrigor
- Kenesil
- Kenzolol
- Modip
- Nidip
- Nimo
- Nimobal
- Nimocal
- Nimodi
- Nimodilat
- Nimodin
- Nimotask
- Nimotop
- Nisom
- Nymalize
- Oxigen
- Periplum
- Tropocer
- Vasoactin
- Vasoflex
- Vasotop
- Vexdipine
Nimodipine Brand Names in Pakistan:
|
Nimodipine Infusion 0.2 mg/ml |
|
|
Bredin |
Medisure Laboratories Pakistan (Pvt.) Ltd. |
|
Nimotop |
Bayer Health Care |
|
Nimodipine Tablets 30 mg |
|
|
Bredin |
Medisure Laboratories Pakistan (Pvt.) Ltd. |
|
Duranim |
Pearl Pharmaceuticals |
|
Nidopin |
Global Pharmaceuticals |
|
Nimoden |
High - Q International |
|
Nimodex |
Mass Pharma (Private) Limited |
|
Nimopro |
Pulse Pharmaceuticals |
|
Nimotin |
Mediate Pharmaceuticals (Pvt) Ltd |
|
Nimotop |
Bayer Health Care |
|
Nimovas |
Spencer Pharma |
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