Acamprosate information from DrugsUpdate
P - Caution when used during pregnancy
Acamprosate is a drug used for treating alcohol dependence.
Acamprosate is thought to stabilize the chemical balance in the brain that would otherwise be disrupted by alcoholism, possibly by blocking glutamatergic N-methyl-D-aspartate receptors, while gamma-aminobutyric acid (GABA) type A receptors are activated.Reports indicate that acamprosate only works with a combination of attending support groups and abstinence from alcohol.Certain serious side effects include allergic reactions, irregular heartbeats, and low or high blood pressure, while less serious side effects include headaches, insomnia, and impotence.Acamprosate should not be taken by people with kidney problems or allergies to the drug.
Pharmacodynamics
Chronic alcohol exposure may alter normal balance between neuronal and excitation and inhibition. In vitro and in vivo animal data suggest acamprosate interacts with glutamate and GABA neurotransmitter systems, restoring this balance.
Pharmacokinetics
Absorption
Bioavailability about 11%. Steady state reached within 5 days. Steady-state concentrations average 350 ng/mL and occur 3 to 8 h postdose. C max and AUC approximately 42% and 23%, respectively.
Distribution
Vd estimated to be 72 to 109 L (1 L/kg). Protein binding is negligible.
Metabolism
Does not undergo metabolism.
Elimination
Terminal t ½ ranges from about 20 to 33 h. Major route of excretion is via kidneys.
Acamprosate Adverse Reactions / Acamprosate Side Effects
Cardiovascular
Palpitation, syncope (at least 1%).
CNS
Insomnia (7%); asthenia, anxiety (6%); depression (5%); dizziness (3%); dry mouth, paresthesia (2%); headache, somnolence, decreased libido, amnesia, abnormal thinking, tremor, vasodilatation, hypertension (at least 1%).
Dermatologic
Pruritus (4%); sweating (2%); rash (at least 1%).
EENT
Pharyngitis, abnormal vision, taste perversion (at least 1%).
GI
Diarrhea (16%); nausea (4%); anorexia, flatulence (3%); vomiting, dyspepsia, constipation, increased appetite (at least 1%).
Genitourinary
Impotence (at least 1%); acute kidney failure (postmarketing).
Metabolic-Nutritional
Peripheral edema, weight gain (at least 1%).
Musculoskeletal
Back pain, myalgia, arthralgia (at least 1%).
Respiratory
Rhinitis, increased cough, dyspnea, bronchitis (at least 1%).
Miscellaneous
Accidental injury, pain (3%); abdominal pain, infection, flu syndrome, chest pain, chills, suicide attempt (at least 1%).
Other Drug Interactions
Antidepressants
Weight gain and loss reported more frequently compared with either agent alone.
Naltrexone
Acamprosate levels may be increased; however, no dosage adjustment is recommended.
List of Contraindications
Acamprosate and Pregnancy
Category C.
Acamprosate and Children
Safety and efficacy not established.
Acamprosate and Geriatic
Because elderly are more likely to have decreased renal function, select dose with care and monitor renal function.
Storage
Store tablets at controlled room temperature (59° to 86°F).
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