Use in Adults
Antihypertensives
THIS GUIDE PROVIDES A PARTIAL LISTING OF PRESCRIBING INFORMATION FOR THIS MEDICATION. FOR A FULL LISTING OF PRESCRIBING INFORMATION PLEASE REFER TO THE PACKAGE INSERT. CLICK ON THE BRAND NAME® TO VIEW THE LINK TO THE PACKAGE INSERT.
ARBs
CANDESARTAN (ATACAND®) NOT FDA APPROVED FOR MIGRAINE PREVENTION CLICK HERE TO EXPAND
Brands:
Initial Dose:
Maintenance Dose:
Suggested Titration Schedule:
Common Side Effects:
Contraindications:
Black Box Warning: Fetal toxicity. Warn women of child-bearing age of the risk for fetal loss if they were to become pregnant and the need for appropriate birth control to prevent pregnancy. Stop therapy when pregnancy is detected.
Pregnancy & Breast Feeding:
Important Drug Interactions:
Initial Dose:
- A common initial dose is 8 mg by mouth daily for those with adequate blood pressures (e.g., systolic blood pressure ≥ 110 mm Hg)
- If blood pressures are lower (e.g., <110 systolic) then may consider 4 mg dose once per day
Maintenance Dose:
- 16 mg by mouth daily
Suggested Titration Schedule:
- Office visit #1:
- Start 8 mgs by month daily
- Consider 4 mg initial dosage in those with low normal blood pressures (e.g., <110 systolic)
- Consider checking a basic metabolic profile 10 days after start to rule out hyperkalemia that can rarely occur with use
- Office visit #2 (2 months later):
- If satisfactory response (e.g., defined as a 50% decrease in the frequency of migraine days per month) then continue current dosage if blood pressure is adequate and no unacceptable side effects
- If unsatisfactory response, consider increasing the dosage to 16 mg by mouth daily if you started with the 8 mg dosage, the blood pressure is adequate and no intolerable side effects
- Increase to 8 mgs by mouth daily if you started with the 4 mg dosage
Common Side Effects:
- Orthostatic hypotension, dizziness; less commonly reported side effects: upper respiratory infections, rhinitis, pharyngitis
- Consider its use in the following groups of patients:
- Those with hypertension and frequent migraine
- Those who have been intolerant of TCAs, beta blockade or topiramate, as candesartan has a low side effect profile.
- Might avoid its use in the following groups of patients:
- Low normal systolic blood pressures (e.g., <100 mm Hg)
- Women of childbearing potential that are not using effective birth control.
- Pregnant women
- Moderate to severe aortic stenosis
- Patients receiving other potassium sparing medications or those at risk for hyperkalemia.
- Advantages are:
- Good efficacy and tolerability as well as modest cost.
- Disadvantages are:
- Teratogenicity in women of childbearing age
- Potential side effect of orthostatic hypotension.
- Lack of formulary coverage. May require a prior authorization.
- Migraine prevention with other angiotensin receptor blockers has not been proven
- Endocrine and metabolic: Hyperkalemia may occur, especially in patients using potassium sparing diuretics, potassium supplements, potassium-containing salt substitutes, or other drugs that raise serum potassium levels; May want to check a basic metabolic profile 10-14 days after its start to check for hyperkalemia and/or rising creatinine
- Cardiovascular: Hypotension may occur, including during major surgery and anesthesia, especially in volume- or salt-depleted patients. Correct volume and salt depletion prior to use and monitor during therapy; dose reduction may be required.
- Concomitant use: avoid use with aliskiren in patients with GFR below 60 mL/min.
- Concomitant use: ACE inhibitor plus mineralocorticoid receptor antagonist is not recommended.
- Hepatic: Moderate hepatic impairment; consider dose reduction.
- Renal: Renal function changes, including acute renal failure, may occur from drugs that inhibit the renin-angiotensin system (RAS), especially in patients whose renal function relies on the RAS (e.g., renal artery stenosis, chronic renal disease, severe heart failure, or volume depletion); monitoring recommended and therapy interruption or discontinuation may be required.
- Special populations: Pediatric patients younger than 1 year; drug may affect kidney development; avoid use for hypertension.
Contraindications:
- Concomitant use with aliskiren in diabetic patients
- Pregnancy
- Fetal loss has been reported with candesartan when administered during pregnancy.
- Stop candesartan when pregnancy is detected.
Black Box Warning: Fetal toxicity. Warn women of child-bearing age of the risk for fetal loss if they were to become pregnant and the need for appropriate birth control to prevent pregnancy. Stop therapy when pregnancy is detected.
Pregnancy & Breast Feeding:
- Click Atacand® and navigate to #8 Use in Specific Populations (8.1 & 8.2)
Important Drug Interactions:
- Aliskren: may result in an increased risk of hyperkalemia, renal impairment, and hypotension.
- ACEs/ARBs: may result in increased risk of adverse events (i.e., hypotension, hyperkalemia, changes in renal function, etc.)
- Trimethoprim/Potassium-sparing drugs: May result in increased risk of hyperkalemia
- Lithium: Increases in serum lithium concentrations and toxicity
- NSAIDS: use may lead to increased risk of renal impairment and loss of antihypertensive effect
- Consider starting a preventive therapy in those with 4 or more migraine days per month.
- Have the patients keep a headache diary to assess the frequency of migraine days per month. This will also help in assessing the response of the preventive medication.
- Counsel patients that it may take 1-4 months after the start of an oral preventive to see an adequate response.
- Set realistic goals with your patients. Explain that a preventive medication is not a cure for migraines. A good response would be a 50% or more reduction in the frequency of migraine days per month. For some patients, a good response may be a significant decrease in the severity of attacks.
- Counsel patients on potential side effects.
- Monitor supine and standing blood pressures if orthostatic symptoms occur.
- Consider checking a basic metabolic profile 10-14 days after its start and periodically thereafter to check for hyperkalemia that rarely can occur with this medication.
CALCIUM-CHANNEL BLOCKERS
VERAPAMIL (CALAN®, ISOPTIN®, VERELAN®) NOT FDA APPROVED FOR MIGRAINE PREVENTION CLICK HERE TO EXPAND
Brands:
Common Side Effects:
Pregnancy & Breast Feeding:
Click Calan® and navigate to #8 Use in Specific Populations (8.1 & 8.2)
Click Isoptin® and navigate to #8 Use in Specific Populations (8.1 & 8.2)
Click Verelan® and navigate to #8 Use in Specific Populations (8.1 & 8.2)
Important Drug Interactions:
- Calan® (verapamil) For Complete Prescribing Information Click Here for the Package Insert
- Isoptin® (verapamil) For Complete Prescribing Information Click Here for the Package Insert
- Verelan® (verapamil) For Complete Prescribing Information Click Here for the Package Insert
- Immediate Release:
- Verapamil 40, 80 and 120 mg tablets
- Might be preferable to use in those with lower blood pressures (e.g., 100 mm Hg or less) as lower dosages can be employed
- Extended Release:
- Verapamil ER (SR) 120, 180 and 240 mg tablets
- Verelan® 120, 180, 240, 360 mg capsules
- Immediate Release
- 40 mg by mouth three times daily
- May start with 40 mg twice per day in those with low blood pressure or in those with medication intolerances
- 40 mg by mouth three times daily
- Extended Release
- 120 mg by mouth one time per day
- 120-360 mgs per day
- Immediate Release
- Office visit #1:
- Start 40 mgs by mouth twice per day during week 1
- Then increase to 40 mg by month three times per day during week 2 if tolerated
- Continue this dosage until office visit #2
- Office visit #2 (2 months later):
- If satisfactory response (e.g., defined as a 50% decrease in the frequency of migraine days per month) then continue current dosage if blood pressure is adequate and no unacceptable side effects.
- If unsatisfactory response, consider gradually increasing the dosage to 80 mg by mouth three times daily if blood pressure is adequate and no intolerable side effects
- Extended Release
- Office visit #1:
- Start 120 mgs by mouth once daily
- Office visit #2 (2 months later):
- If satisfactory response (e.g., defined as a 50% decrease in the frequency of migraine days per month) then continue current dosage if blood pressure is adequate and no unacceptable side effects
- If unsatisfactory response, then consider increasing the dosage to 240 mgs once daily if blood pressure is adequate and no intolerable side effects
Common Side Effects:
- Bradycardia, dizziness upon standing, constipation
- The level of evidence supporting its use as a migraine preventive is not as strong as many other medications.
- Consider use in those that have:
- Auras
- Appears to work better in those that have auras (e.g., visual, sensory, motor or speech auras)
- Considered the preventive medication of choice in those with hemiplegic migraine by many headache specialists.
- Raynaud’s disease
- IBS-D (diarrhea predominant irritable bowel syndrome)
- May be effective in those with cluster headache that also have attacks of migraine
- Auras
- Might consider an electrocardiogram in elderly patients and in those with cardiac disease as verapamil can prolong the PR interval and cause heart block.
- Main advantage is:
- Its efficacy in those with aura, a long track record of safety and low cost.
- Main disadvantages are:
- Constipation. Avoid in those with moderate to severe constipation.
- Avoid those with low normal systolic blood pressures (e.g., <100 mm Hg).
- Heart disease: In patients with left ventricular systolic dysfunction, use of verapamil may result in acute decompensation and deterioration with development of pulmonary edema and/or hypotension. Acute cardiac failure associated with verapamil in patients with no prior history of chronic heart failure have also been reported
- Slow Heart Rate: Verapamil may cause first-, second-, or third-degree atrioventricular (AV) block or sinus bradycardia
- Atrial fibrillation/flutter associated with accessory bypass tract (e.g., Wolff-Parkinson-White, Lown-Ganong-Levine)
- Cardiogenic shock
- Hypotension (less than 90 mmHg systolic pressure)
- Left ventricular dysfunction, severe (ejection fraction less than 30%)
- Second- or third-degree atrioventricular block (without functioning artificial pacemaker)
- Sick sinus syndrome (without functioning artificial pacemaker) [21][22]
Pregnancy & Breast Feeding:
Click Calan® and navigate to #8 Use in Specific Populations (8.1 & 8.2)
Click Isoptin® and navigate to #8 Use in Specific Populations (8.1 & 8.2)
Click Verelan® and navigate to #8 Use in Specific Populations (8.1 & 8.2)
Important Drug Interactions:
- Alcohol (Ethanol): Verapamil may increase the serum concentration of alcohol (ethyl).
- Alprazolam: CYP3A4 inhibitors (moderate) may increase the serum concentration of alprazolam. Management: Consider alternatives to this combination when possible. If combined, consider an alprazolam dose reduction, and monitor for increased alprazolam effects and toxicities (e.g., sedation, lethargy).
- 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]).
- Aripiprazole: CYP3A4 Inhibitors (moderate) may increase the serum concentration of aripiprazole. Management: Monitor for increased aripiprazole pharmacologic effects. Aripiprazole dose adjustments may or may not be required based on concomitant therapy, indication, or dosage form.
- Aspirin: Calcium channel blockers (non-dihydropyridine) may enhance the antiplatelet effect of aspirin.
- Barbiturates: May enhance the hypotensive effect of blood pressure lowering agents.
- Ergot derivatives: CYP3A4 inhibitors (moderate) may increase the serum concentration of ergot derivatives.
- Consider starting a preventive therapy in those with 4 or more migraine days per month.
- Have the patients keep a headache diary to assess the frequency of migraine days per month. This will also help in assessing the response of the preventive medication.
- Counsel patients that it may take 1-4 months after the start of an oral preventive to see an adequate response.
- Set realistic goals with your patients. Tell them that a preventive medication is not a cure for migraines. A good response would be a 50% or more reduction in the frequency of migraine days per month.
- Counsel patients on side effects or they may discontinue the medication.
- Taking verapamil SR in the evening may minimize orthostatic side effects
BETA-BLOCKERS
Propranolol (Inderal®, Innopran®) FDA APPROVED FOR MIGRAINE PREVENTION Click Here to expand
Brands:
Contraindications:
Pregnancy & Breast Feeding:
- INDERAL®, (propranolol) For Complete Prescribing Information Click Here for the Package Insert
- INNOPRAN®, (propranolol) For Complete Prescribing Information Click Here for the Package Insert
- Immediate release:
- Propranolol 10, 20, 40, 60, 80 mg tabs
- Extended Release
- Inderal LA 60, 80, 120 mg capsules
- Inderal ER 160 mg capsule
- InnoPran XL 80, 120 mg capsules
- 20-80 mg by mouth per day
- May use either immediate (IR) or extended release (ER) formulations
- Immediate release is generally preferred in patients with lower blood pressures (e.g., <110 systolic), lower pulse rates, or intolerances to a lot of medications as lower dosages are available.
- 20-160 mg by mouth per day
- Immediate Release (IR) Formulation:
- Office visit #1:
- Start at 10 mgs at night during week 1
- Then increase to 10 mgs two times per day during week 2
- If tolerated, increase to 10 mgs in the morning and 20 mgs in the evening during week 3
- During the 4th week increase to 20 mg in the morning and 20 mgs in the evening if tolerated
- Remain on that dosage until office visit #2
- Office visit #2 (2 months later):
- if satisfactory response (e.g., defined as a 50% decrease in the frequency of migraine days per month) then continue current dosage if blood pressure and pulse are adequate and no unacceptable side effects
- If unsatisfactory response, then consider increasing the dosage gradually to 40 mg by mouth twice daily if blood pressure and pulse are adequate and no intolerable side effects
- Extended Release (ER) Formulation:
- Office Visit #1:
- Start at 60-80 mgs by mouth daily
- Office visit #2 (2 months later):
- If satisfactory response (e.g., defined as a 50% decrease in the frequency of migraine days per month) then continue current dosage if blood pressure and pulse are adequate and no unacceptable side effects
- If unsatisfactory response, then consider increasing the dosage to 120 mgs by month per day if blood pressure and pulse are adequate and no intolerable side effects
- Office Visit #1:
- Fatigue, insomnia, vivid dreams, sexual disorder, orthostatic hypotension, hypotension, exercise intolerance
- Can be used as a “first line” preventive, a group of medications commonly recommended as initial therapy in those starting a preventive for the first time.
- Tricyclic antidepressants, beta blockers and topiramate are also considered “first line” preventives.
- Consider use in the following patient populations:
- Those with migraine and concurrent hypertension
- Those with postural orthostatic tachycardia syndrome (POTS syndrome)
- Those with essential tremor
- Those with comorbid anxiety disorders
- Consider avoiding in following patient populations:
- Those with systolic blood pressures less than 100 mm Hg
- Those with asthma, chronic obstructive pulmonary disease (COPD), cardiac conduction disease and congestive heart failure.
- Those receiving medications that block AV conduction such as some calcium channel blocker
- Those with aggressive exercise regimens
- Consider checking an EKG an electrocardiogram (EKG) to rule out AV block in the elderly and in those with known cardiac disease.
- Main advantages are:
- Good efficacy, long track record of safety and low cost.
- Main disadvantages are:
- Side effects of fatigue and orthostasis
- Need to avoid in patients with blood pressures in the low normal range (e.g., systolic bp <100 mm Hg)
- Hypoglycemia: Rarely beta-blockers have been associated with hypoglycemia. In addition, they may mask hypoglycemia symptoms in those with diabetes (except for sweating).
- Bronchospasm: Bronchospasm can occur with use of beta-blockers in those with chronic obstructive pulmonary disease and asthma.
- Bradycardia: Beta-blockers have been associated with bradyarrhythmia. Avoid in patients with atrioventricular blockage. It may be necessary to check an electrocardiogram before use in the elderly and other high risk patient groups to rule out a prolonged PR interval that would contraindicate its use
- Abrupt discontinuation: Abrupt discontinuation of beta blockers has been associated with myocardial infarction or acute cardiac syndromes (e.g., unstable angina) particularly in those with preexisting coronary artery disease. It is recommended to slowly decrease these medications when discontinued to prevent these events.
- Comorbid illnesses: Cautious use in those with congestive heart failure, hepatic, or renal disease, asthma, or diabetes
Contraindications:
- Systolic blood pressure less than 100 mmHg
- History of bronchial asthma or bronchospasm
- Cardiogenic shock or decompensated heart failure
- Heart rate less than 60 beats/min
- Pheochromocytoma
- Second- or third-degree heart block (if no pacemaker is present)
- Sick sinus syndrome (if no pacemaker is present)
- Sinus bradycardia (if no pacemaker is present)
Pregnancy & Breast Feeding:
- Click INDERAL® and navigate to #8 Use in Specific Populations (8.1 & 8.2)
- Click INNOPRAN® and navigate to #8 Use in Specific Populations (8.1 & 8.2)
- Alcohol (Ethyl): May increase or decrease the serum concentration of propranolol.
- Amphetamines: May diminish the antihypertensive effect of antihypertensive agents.
- Antipsychotic Agents (Phenothiazines): May enhance the hypotensive effect of beta-blockers. Concurrent use of phenothiazines and beta-blockers may result in increased levels of both medications.
- 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.
- Cannabis: May decrease the serum concentration of CYP1A2 substrates (high risk with inducers).
- Cholinergic Agonists: Beta-blockers may enhance the adverse/toxic effect of cholinergic agonists. Of particular concern are the potential for cardiac conduction abnormalities and bronchoconstriction.
- CYP1A2 Inhibitors (Strong): May increase the serum concentration of propranolol. Management: Use a lower initial propranolol dose and be more cautious during propranolol dose titration if combined with strong CYP1A2 inhibitors.
- CYP2D6 Inhibitors (Strong): May increase the serum concentration of propranolol.
- Duloxetine: Blood Pressure Lowering Agents may enhance the hypotensive effect of duloxetine.
- Ergot Derivatives (Vasoconstrictive CYP3A4 Substrates): Beta-Blockers may enhance the vasoconstricting effect of ergot derivatives (vasoconstrictive CYP3A4 substrates).
- Herbal Products with Blood Pressure Increasing Effects: May diminish the antihypertensive effect of antihypertensive agents.
- Herbal Products with Blood Pressure Lowering Effects: May enhance the hypotensive effect of blood pressure lowering agents.
- Insulin: Beta blockers may enhance the hypoglycemic effect of all forms of insulin.
- Nonsteroidal Anti-Inflammatory Agents: May diminish the antihypertensive effect of beta blockers.
- Rizatriptan: Propranolol may increase the serum concentration of rizatriptan. Management: For adults, limit rizatriptan dose to 5 mg (maximum of 3 doses per 24 hours). For pediatric patients, if weight is 40 kg or more, limit rizatriptan to a single 5 mg dose per 24 hours; do not combine both drugs, if weight is less than 40 kg.
- Tizanidine: CYP1A2 Inhibitors (weak) may increase the serum concentration of tizanidine. Management: Avoid these combinations when possible. If combined use is necessary, initiate tizanidine at an adult dose of 2 mg per day and increase in 2 to 4 mg increments based on patient response. Monitor for increased effects of tizanidine, including adverse reactions.
- Tobacco (Smoked): May decrease the serum concentration of propranolol.
- Consider starting a preventive therapy in those with 4 or more migraine days per month.
- Have the patients keep a headache diary to assess the frequency of migraine days per month. This will also help in assessing the response of the preventive medication.
- Counsel patients that it may take 1-4 months after the start of an oral preventive to see an adequate response.
- Set realistic goals with your patients. Explain that a preventive medication is not a cure for migraines, but a means of controlling migraine frequency and severity. A good response would be a 50% or more reduction in the frequency of migraine days per month and often a corresponding reduction in severity of attacks.
- Counsel patients on potential side effects, so that they will not be frightened or concerned if side effects occur, which otherwise might prompt them to discontinue.
Timolol (Blocadren®) FDA APPROVED FOR MIGRAINE PREVENTION CLICK HERE TO EXPAND
Brands:
Contraindications:
Pregnancy & Breast Feeding:
Click Blocadren® and navigate to #8 Use in Specific Populations (8.1 & 8.2)
Important Drug Interactions:
- Blocadren® (timolol) For Complete Prescribing Information Click Here for the Package Insert NOT FOUND
- 5, 10, 20 mg tablets
- 10 mg by mouth daily
- 10 mg by mouth twice daily (max 30 mg per day)
- Office visit #1:
- 10 mg by mouth daily for 2 weeks
- Then if tolerated, increase to 10 mg by mouth two times per day
- Continue this dosage until office visit #2
- Office visit #2 (2 months later):
- If satisfactory response (e.g., defined as a 50% decrease in the frequency of migraine days per month) then continue current dosage if blood pressure and pulse are adequate and no unacceptable side effects
- If unsatisfactory response, then consider increasing the dosage to 20 mgs po in the morning and 10 mg po in the evening (total dose 30 mg per day) if blood pressure and pulse are adequate and no intolerable side effects
- Fatigue, insomnia, vivid dreams, sexual disorder, orthostatic symptoms (dizziness on going from a sitting to a standing position), hypotension, exercise intolerance
- Timolol represents a “first line” preventive, a group of medications commonly recommended as initial therapy in those starting a preventive for the first time.
- Tricyclic antidepressants, beta blockers and topiramate are also considered “first line” preventives.
- Consider use in the following patient populations:
- Those with migraine and concurrent hypertension
- Those with postural orthostatic tachycardia syndrome (POTS syndrome)
- Those with co-existing essential tremor or generalized anxiety or performance anxiety.
- Avoid in the following patient populations:
- Those with systolic blood pressures less than 100 mm Hg
- Those with asthma, chronic obstructive pulmonary disease (COPD), cardiac conduction disease and congestive heart failure, and diabetes.
- Those receiving medications that block AV conduction, such as some calcium channel blockers
- Consider obtaining an electrocardiogram (EKG) to ensure no AV block is present, particularly in the elderly and in those with known cardiac disease.
- Main advantages are:
- good efficacy, long track record of safety and low cost
- Main disadvantages are:
- Side effects of fatigue, exercise intolerance, orthostasis.
- Avoid in patients with blood pressures in the low normal range (e.g., systolic bp <100 mm Hg) as they are at particularly high risk for orthostatic symptoms and fatigue.
- Impaired Hepatic or Renal Function: Since timolol is partially metabolized in the liver and excreted mainly by the kidneys, dosage reductions may be necessary when hepatic and/or renal insufficiency is present.
- Dosing in the Presence of Marked Renal Failure: Although the pharmacokinetics of timolol are not greatly altered by renal impairment, marked hypotensive responses have been seen in patients with marked renal impairment undergoing dialysis after 20 mg doses. Dosing in such patients should therefore be especially cautious.
- Muscle Weakness: Beta-adrenergic blockade has been reported to potentiate muscle weakness consistent with certain myasthenic symptoms (e.g., diplopia, ptosis, and generalized weakness). Timolol has been reported rarely to increase muscle weakness in some patients with myasthenia gravis or myasthenic symptoms.
Contraindications:
- Active or history of bronchial asthma
- Cardiogenic shock
- Overt cardiac failure
- Second- or third-degree atrioventricular block
- Severe COPD
- Sinus bradycardia
Pregnancy & Breast Feeding:
Click Blocadren® and navigate to #8 Use in Specific Populations (8.1 & 8.2)
Important Drug Interactions:
- Catecholamine-Depleting Drugs: Possible additive effects and the production of hypotension and/or marked bradycardia, which may produce vertigo, syncope, or postural hypotension.
- Non-Steroidal Anti-Inflammatory Drugs: Blunting of the antihypertensive effect of beta-adrenoceptor blocking agents by non-steroidal anti-inflammatory drugs has been reported. When using these agents concomitantly, patients should be observed carefully to confirm that the desired therapeutic effect has been obtained.
- Digitalis and Either Diltiazem or Verapamil: The concomitant use of beta-adrenergic blocking agents with digitalis and either diltiazem or verapamil may have additive effects in prolonging AV conduction time.
- Quinidine: Potentiated systemic beta-blockade (e.g., decreased heart rate) has been reported during combined treatment with quinidine and timolol, possibly because quinidine inhibits the metabolism of timolol via the P-450 enzyme, CYP2D6.
- Clonidine: Beta-adrenergic blocking agents may exacerbate the rebound hypertension which can follow the withdrawal of clonidine
- Consider starting a preventive therapy in those with 4 or more migraine days per month.
- Have the patients keep a headache diary to assess the frequency of migraine days per month. This will also help in assessing the response of the preventive medication.
- Counsel patients that it may take 1-4 months after the start of an oral preventive to see an adequate response.
- Set realistic goals with your patients. Tell them that a preventive medication is not a cure for migraines. A good response would be a 50% or more reduction in the frequency of migraine days per month.
- Counsel patients on side effects or they may discontinue the medication.
MEtoprolol (Lopressor®, Toprol®) NOT FDA APPROVED FOR MIGRAINE PREVENTION CLICK HERE TO EXPAND
Brands:
Common Side Effects:
Contraindications:
Pregnancy & Breast Feeding:
Important Drug Interactions:
- Lopressor® (metoprolol) For Complete Prescribing Information Click Here for the Package Insert
- Toprol®XL (metoprolol) For Complete Prescribing Information Click Here for the Package Insert
- Immediate Release
- Metoprolol tartrate 25, 50 and 100 mg tablets
- Immediate release is generally preferred in patients with lower blood pressures (e.g., <110 systolic), lower pulse rates, or intolerances to a lot of medications as lower dosages are available.
- Extended Release
- Metoprolol tartrate 25, 50 and 100 mg tablets
- Has not been studied in those with migraine
- Immediate Release
- 25 mg by mouth twice daily
- Might consider starting with 25 mgs once in the morning for those with medication intolerances or lower blood pressure
- Extended Release
- 50 mgs by month once daily
- 50-200 mg per day
- Immediate Release
- Office visit #1:
- Start 25 mgs by mouth once in the morning for the first week
- Then increase to 25 mgs two times per day if tolerated after first week
- Continue this dosage until office visit #2
- Office visit #2 (2 months later):
- If satisfactory response (e.g., defined as a 50% decrease in the frequency of migraine days per month) then continue current dosage if blood pressure and pulse are adequate and no unacceptable side effects
- If unsatisfactory response, consider increasing the dosage to 50 mgs by mouth two times per day if blood pressure and pulse are adequate and no intolerable side effects insomnia, vivid dreams, impotence, orthostatic symptoms
- Extended Release
- Office visit #1:
- Start 50 mgs by mouth one time per day
- Office visit #2 (2 months later):
- If satisfactory response (e.g., defined as a 50% decrease in the frequency of migraine days per month) then continue current dosage if blood pressure and pulse are adequate and no unacceptable side effects
- If unsatisfactory response, then consider increasing the dosage to 100 mgs by mouth one time per day if blood pressure and pulse are adequate and no intolerable side effects
Common Side Effects:
- Fatigue, orthostatic symptoms (dizziness on going from a sitting to a standing position), hypotension; less common: impotence, vivid dreams, insomnia
- Can be used as a “first line” preventive, a group of medications commonly recommended as initial therapy in those starting a preventive for the first time.
- Tricyclic antidepressants, beta blockers and topiramate are considered “first line” preventives.
- Consider use in the following patient populations:
- Those with migraine and concurrent hypertension
- Those with postural orthostatic tachycardia syndrome (POTS syndrome)
- Those with essential tremor or comorbid anxiety
- Consider avoiding in following patient populations:
- Those with systolic blood pressures less than 100 mm Hg
- Those with asthma, chronic obstructive pulmonary disease (COPD), cardiac conduction disease and congestive heart failure.
- Those receiving medications that block AV conduction such as some calcium channel blocker
- Consider checking an EKG an electrocardiogram (EKG) to rule out AV block in the elderly and in those with known cardiac disease.
- Main advantages are:
- Good efficacy, long track record of safety and low cost.
- Main disadvantages are:
- Side effects of fatigue and orthostasis.
- Avoid in patients with blood pressures in the low normal range (e.g., systolic bp <100 mm Hg) as they maybe at higher risk for orthostatic symptoms and fatigue.
- Cardiovascular: Heart failure may worsen during dosage increases; dosage adjustment or interruption may be needed. May cause or aggravate symptoms of arterial insufficiency in patients with peripheral vascular disease
- Endocrine and metabolic: Use in pheochromocytoma can be associated with a paradoxical increase in blood pressure if alpha blockade is not initiated. Use in patients with diabetes may mask tachycardia occurring with hypoglycemia. Use may mask clinical signs of hyperthyroidism such as tachycardia.
- Hepatic: Dosage adjustment may be necessary, and monitoring recommended with hepatic impairment
- Respiratory: Use not recommended in bronchospastic disease unless intolerant of or refractory to other antihypertensives; dosage adjustment necessary
Contraindications:
- Cardiogenic shock
- Decompensated cardiac failure
- Hypersensitivity to metoprolol succinate or any component of the product
- Second- or third-degree heart block
- Severe bradycardia
- Sick sinus syndrome (without a functional permanent pacemaker)
Pregnancy & Breast Feeding:
- Click Lopressor® and navigate to #8 Use in Specific Populations (8.1 & 8.2)
- Click Toprol® and navigate to #8 Use in Specific Populations (8.1 & 8.2)
Important Drug Interactions:
- Acetylcholinesterase Inhibitors: May enhance the bradycardic effect of beta blockers.
- Alpha1-Blockers: Beta blockers may enhance the orthostatic hypotensive effect of alpha1 blockers.
- Amphetamines: May diminish the antihypertensive effect of antihypertensive agents.
- Antipsychotic Agents (Phenothiazines): May enhance the hypotensive effect of beta blockers. Beta blockers may decrease the metabolism of antipsychotic agents (phenothiazines). Antipsychotic agents (phenothiazines) may decrease the metabolism of beta blockers.
- Antipsychotic Agents (Second Generation [Atypical]): Blood pressure lowering agents may enhance the hypotensive effect of antipsychotic agents (second generation [atypical]).
- Alpha2-Agonists: May enhance the AV-blocking effect of beta blockers.
- Duloxetine: Blood pressure lowering agents may enhance the hypotensive effect of duloxetine.
- Consider starting a preventive therapy in those with 4 or more migraine days per month.
- Have the patients keep a headache diary to assess the frequency of migraine days per month. This will also help in assessing the response of the preventive medication.
- Counsel patients that it may take 1-4 months after the start of an oral preventive to see an adequate response.
- Set realistic goals with your patients. Explain that a preventive medication is not a cure for migraines. A good response after starting treatment would be a 50% or more reduction in the frequency of migraine days per month. Other responses may include a reduction in severity of attacks.
- Counsel patients on side effects, most common and likely strategies for addressing.
- Warn patients to avoid activities requiring mental alertness or coordination until drug effects are realized, as drug may cause dizziness.
- Advise diabetic patients to carefully monitor blood glucose as drug may mask symptoms of hypoglycemia.
- Patients should take extended-release tablets with or immediately following meals.
- Counsel patients against sudden discontinuation of drug, as this may precipitate hypertension, angina, or myocardial infarction.
Nadolol (Corgard®) NOT FDA APPROVED FOR MIGRAINE PREVENTION CLICK HERE TO EXPAND
Brands: Available Dosages:
Contraindications:
Pregnancy & Breast Feeding:
Important Drug Interactions:
- 20, 40 and 80 mg tablets
- 20 mg by mouth once daily
- 40-240 mg by mouth once daily
- Office visit #1:
- Start with 20 mg by mouth once daily
- Office visit #2 (2 months later):
- If satisfactory response (e.g., defined as a 50% decrease in the frequency of migraine days per month) then continue current dosage if blood pressure and pulse are adequate and no unacceptable side effects
- If unsatisfactory response, consider increasing the dosage to 40 mg once daily if blood pressure and pulse are adequate and no intolerable side effects
- Depression, fatigue, orthostasis, lightheadedness, dizziness, bradyarrhythmia
- Can be used as a “first line” preventive, a group of medications that is commonly recommended as initial therapy in those starting a preventive for the first time.
- Tricyclic antidepressants, beta blockers and topiramate are considered “first line” preventives.
- Consider use in the following patient populations:
- Those with migraine and concurrent hypertension
- Those with postural orthostatic tachycardia syndrome (POTS syndrome), essential tremor or generalized anxiety disorders
- Consider avoiding in following patient populations:
- Those with systolic blood pressures less than 100 mm Hg
- Those with asthma, chronic obstructive pulmonary disease (COPD), cardiac conduction disease and congestive heart failure.
- Those receiving medications that block AV conduction such as some calcium channel blocker
- Consider checking an EKG an electrocardiogram (EKG) to rule out AV block in the elderly and in those with known cardiac disease.
- Main advantages are:
- Good efficacy, long track record of safety and low cost.
- Main disadvantages are:
- Side effects of fatigue and orthostasis.
- Avoid in patients with blood pressures in the low normal range (e.g., systolic bp <100 mm Hg) as they may be at higher risk for orthostatic symptoms and fatigue.
- Cardiovascular: Inhibition of sympathetic stimulation increases potential for new-onset or worsening of well-compensated heart failure; monitoring recommended and discontinuation may be necessary.
- Endocrine and Metabolic: Release of insulin may be reduced, resulting in hyperglycemia. May mask symptoms associated with hypoglycemia (e.g., tachycardia and blood pressure changes). May mask clinical signs of hyperthyroidism, such as tachycardia.
- Renal: Use with caution in patients with renal impairment; dosage adjustment necessary.
- Respiratory: May block bronchodilation in patients with bronchospastic disease (e.g., chronic bronchitis, emphysema); use not recommended.
Contraindications:
- Active or history of bronchial asthma
- Cardiogenic shock
- Overt cardiac failure
- Second- or third-degree atrioventricular block
- Severe COPD
- Sinus bradycardia
Pregnancy & Breast Feeding:
- Click Corgard® and navigate to #8 Use in Specific Populations (8.1 & 8.2)
Important Drug Interactions:
- Beta2-Agonists: Beta blockers (non-selective) may diminish the bronchodilator effect of Beta2 agonists.
- Lasmiditan: May increase the serum concentration of P-glycoprotein/ABCB1 Substrates (high risk with inhibitors).
- Acetylcholinesterase Inhibitors: May enhance the bradycardic effect of beta blockers.
- Alpha1-Blockers: Beta blockers may enhance the orthostatic hypotensive effect of alpha-1 blockers.
- Amphetamines: May diminish the antihypertensive effect of antihypertensive agents.
- Antipsychotic Agents (Phenothiazines): May enhance the hypotensive effect of beta blockers. Beta blockers may decrease the metabolism of antipsychotic agents (phenothiazines). Antipsychotic agents (phenothiazines) may decrease the metabolism of Beta blockers.
- Antipsychotic Agents (Second Generation [Atypical]): Blood pressure lowering agents may enhance the hypotensive effect of antipsychotic agents (Second Generation [Atypical]).
- Alpha2-Agonists: May enhance the AV-blocking effect of beta blockers.
- Duloxetine: Blood pressure lowering agents may enhance the hypotensive effect of duloxetine.
- Consider starting a preventive therapy in those with 4 or more migraine days per month.
- Have the patients keep a headache diary to assess the frequency of migraine days per month. This will also help in assessing the response of the preventive medication.
- Counsel patients that it may take 1-4 months after the start of an oral preventive to see an adequate response.
- Set realistic goals with your patients. Explain that a preventive medication is not a cure for migraines. A good response would be a 50% or more reduction in the frequency of migraine days per month.
- Counsel patients on side effects or they may discontinue the medication. Other benefits may be a reduction in the severity of attacks.
- Side effects may include abdominal discomfort, constipation, or diarrhea.
- Drugs may mask symptoms of hypoglycemia. Diabetic patients may need to closely monitor blood glucose.
- Advise patients against sudden discontinuation of drug, as this may exacerbate angina, cause rebound hypertension, or induce a myocardial infarction. Instruct the patient to take a missed dose as soon as possible, but if the next dose is in less than 8 h, skip the missed dose.
Atenolol (Tenormin®) NOT FDA APPROVED FOR MIGRAINE PREVENTION CLICK HERE TO EXPAND
Brands: Available Dosages:
Contraindications:
Pregnancy & Breast Feeding:
Important Drug Interactions:
- 25, 50 and 100 mg tablets
- 25 mg once in the morning
- Might start with 12.5 mg (1/2 of a 25 mg tab) in those with lower blood pressures (e.g., <110 systolic) or in those with multiple medication intolerances
- 12.5-100 mg by mouth once daily
- Office visit #1:
- Start with 25 mg by mouth once daily
- Office visit #2 (2 months later):
- If satisfactory response (e.g., defined as a 50% decrease in the frequency of migraine days per month) then continue current dosage if blood pressure and pulse are adequate and no unacceptable side effects
- If unsatisfactory response, consider increasing the dosage to 50 mg once daily if blood pressure and pulse are adequate and no intolerable side effects
- Depression, fatigue, orthostasis, lightheadedness, dizziness, bradyarrhythmia
- Can be used as a “first line” preventive, a group of medications that is commonly recommended as initial therapy in those starting a preventive for the first time.
- Tricyclic antidepressants, beta blockers and topiramate are considered “first line” preventives.
- Consider use in the following patient populations:
- Those with migraine and concurrent hypertension
- Those with postural orthostatic tachycardia syndrome (POTS syndrome), essential tremor or generalized anxiety disorders
- Consider avoiding in following patient populations:
- Those with systolic blood pressures less than 100 mm Hg
- Those with asthma, chronic obstructive pulmonary disease (COPD), cardiac conduction disease and congestive heart failure.
- Those receiving medications that block AV conduction such as some calcium channel blocker
- Consider checking an EKG an electrocardiogram (EKG) to rule out AV block in the elderly and in those with known cardiac disease.
- Main advantages are:
- Good efficacy, long track record of safety and low cost.
- Main disadvantages are:
- Side effects of fatigue and orthostasis.
- Avoid in patients with blood pressures in the low normal range (e.g., systolic bp <100 mm Hg) as they may be at higher risk for orthostatic symptoms and fatigue.
- Cardiovascular: Inhibition of sympathetic stimulation increases potential for new-onset or worsening of well-compensated heart failure; monitoring recommended and discontinuation may be necessary.
- Endocrine and Metabolic: Release of insulin may be reduced, resulting in hyperglycemia. May mask symptoms associated with hypoglycemia (e.g., tachycardia and blood pressure changes). May mask clinical signs of hyperthyroidism, such as tachycardia.
- Renal: Use with caution in patients with renal impairment; dosage adjustment necessary.
- Respiratory: May block bronchodilation in patients with bronchospastic disease (e.g., chronic bronchitis, emphysema); use not recommended.
Contraindications:
- Active or history of bronchial asthma
- Cardiogenic shock
- Overt cardiac failure
- Second- or third-degree atrioventricular block
- Severe COPD
- Sinus bradycardia
Pregnancy & Breast Feeding:
- Click Tenormin® and navigate to #8 Use in Specific Populations (8.1 & 8.2)
Important Drug Interactions:
- Beta2-Agonists: Beta blockers (non-selective) may diminish the bronchodilator effect of Beta2 agonists.
- Lasmiditan: May increase the serum concentration of P-glycoprotein/ABCB1 Substrates (high risk with inhibitors).
- Acetylcholinesterase Inhibitors: May enhance the bradycardic effect of beta blockers.
- Alpha1-Blockers: Beta blockers may enhance the orthostatic hypotensive effect of alpha-1 blockers.
- Amphetamines: May diminish the antihypertensive effect of antihypertensive agents.
- Antipsychotic Agents (Phenothiazines): May enhance the hypotensive effect of beta blockers. Beta blockers may decrease the metabolism of antipsychotic agents (phenothiazines). Antipsychotic agents (phenothiazines) may decrease the metabolism of Beta blockers.
- Antipsychotic Agents (Second Generation [Atypical]): Blood pressure lowering agents may enhance the hypotensive effect of antipsychotic agents (Second Generation [Atypical]).
- Alpha2-Agonists: May enhance the AV-blocking effect of beta blockers.
- Duloxetine: Blood pressure lowering agents may enhance the hypotensive effect of duloxetine.
- Consider starting a preventive therapy in those with 4 or more migraine days per month.
- Have the patients keep a headache diary to assess the frequency of migraine days per month. This will also help in assessing the response of the preventive medication.
- Counsel patients that it may take 1-4 months after the start of an oral preventive to see an adequate response.
- Set realistic goals with your patients. Explain that a preventive medication is not a cure for migraines. A good response would be a 50% or more reduction in the frequency of migraine days per month.
- Counsel patients on side effects or they may discontinue the medication. Other benefits may be a reduction in the severity of attacks.
- Side effects may include abdominal discomfort, constipation, or diarrhea.
- Drugs may mask symptoms of hypoglycemia. Diabetic patients may need to closely monitor blood glucose.
- Advise patients against sudden discontinuation of drug, as this may exacerbate angina, cause rebound hypertension, or induce a myocardial infarction. Instruct the patient to take a missed dose as soon as possible, but if the next dose is in less than 8 h, skip the missed dose.