cimetidine (Rx)

Brand and Other Names:Tagamet HB
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Dosing & Uses

AdultPediatricGeriatric

Dosage Forms & Strengths

injectable solution

  • 150mg/mL

oral solution

  • 300mg/5mL

tablet

  • 200mg
  • 300mg
  • 400mg (Rx)
  • 600mg (Rx)
  • 800mg (Rx)
more...

Benign Gastric Ulcer

800 mg PO qHS OR

400 mg PO q12hr OR

300 mg PO q6hr

Duodenal Ulcer

800 mg PO qHS OR

400 mg PO q12hr OR

300 mg PO q6hr

Erosive Gastroesophageal Reflux Disease

800 mg PO q12hr OR

400 mg PO q6hr

Heartburn

Over the counter only

To relieve symptoms: 200 mg PO up to q12hr

To prevent symptoms: 200 mg PO with glass of water right before or any time up to 30 minutes before eating food or drinking beverages that cause heartburn

Pathological Hypersecretory Conditions

300 mg PO q6hr with meals and HS

Renal Impairment

CrCl<30 mL/min

300 mg IV/IO q12hr

Prevention of upper GI bleeding: 25 mg/hour continuous IV infusion

Other Indications & Uses

PUD (treatment, maintenance), gastric ulcer treatment, GI bleeding prevention in critically ill patients, hypersecretory conditions (e.g., Zollinger-Ellison)

Dosage Forms & Strengths

injectable solution

  • 150mg/mL

oral solution

  • 300mg/5mL

tablet

  • 200mg
  • 300mg
  • 400mg (Rx)
  • 600mg (Rx)
  • 800mg (Rx)
more...

Duodenal Ulcer (Off-label)

<16 years: Use only if benefit outweighs risks

20-40 mg/kg/day IV/PO divided q6hr 

Neonates (<28 days old): 5-20 mg/kg/day IV/PO divided q8-12hr

Infants: 10-20 mg/kg/day IV/PO divided q6-12hr

Not drug of choice in elderly because of increased potential for confusion and drug interactions

Benign Gastric Ulcer

800 mg PO qHS OR

400 mg PO q12hr OR

300 mg PO q6hr

Duodenal Ulcer

800 mg PO qHS OR

400 mg PO q12hr OR

300 mg PO q6hr

Erosive Gastroesophageal Reflux Disease

800 mg PO q12hr OR

400 mg PO q6hr

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Interactions

Interaction Checker

and cimetidine

No Results

     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse Effects

            1-10%

            Headache (2.1%)

            Dizziness (1%)

            Somnolence (1%)

            Gynecomastia (0.3-4%)

            Frequency Not Defined

            Confusion (elderly)

            Impotence

            Diarrhea

            Nausea

            Vomiting

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            Warnings

            Contraindications

            Hypersensitivity to cimetidine or other H2 receptor antagonists

            Cautions

            Antiandrogen: may cause feminization & sexual dysfunction in males

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            Pregnancy & Lactation

            Pregnancy Category: B

            Lactation: enters breast milk/not recommended

            Pregnancy Categories

            A:Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

            B:May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

            C:Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

            D:Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

            X:Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

            NA:Information not available.

            more...
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            Pharmacology

            Mechanism of Action

            H2-receptor antagonist; blocks H2-receptors of gastric parietal cells, leading to inhibition of gastric secretions

            Pharmacokinetics

            Bioavailability: PO: 60-70% (undergoes minimal 1st pass metabolism)

            Protein Bound: 15-20%

            Metabolism: Liver, inhibit microsomal enzymes

            Metabolites: Cimetidine sulfoxide, 5-hydroxymethyl derivative (inactive met)

            Dialyzable: Yes, removed by HD and PD

            Enzymes inhibited: hepatic CYP1A2, CYP2D6, CYP3A4

            Half-Life

            • Adults: 2 hr; increases to 4-5 hr with renal impairment
            • Infant: 2.1-3.6 hr

            Onset

            • IV: 30 min
            • PO: <1 hr

            Duration

            • IV/IM: 4-5 hr
            • PO: 4-8 hr

            Peak Plasma Time

            • IM: 15 min
            • PO: 45-90 min

            Vd

            • Adults: 1 L/kg
            • Children 1-12 years: 2.13 L/kg

            Clearance

            • Total Body: 30-48 L/hr
            • Renal: 13.8-30 L/hr (removed by HD & PD)

            Excretion

            • Urine: 48-75%
            • Feces: 2-3% (<2% in bile)
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            Administration

            IV/IM Administration

            Administered IM with no dilution, OR

            Slow direct IV injection over 5 min or more after dilution to a total of 20 mL with compatible diluent (NS), OR

            Intermittent IV infusion over 15 to 20 min in at least 50 mL of compatible diluent, OR

            Continuous IV infusion in 100 to 1000 mL of compatible diluent over 24 hr

            IV Compatibilities

            Additive: cefazolin, clindamycin, epinephrine, erythromycin, furosemide, gentamicin, lidocaine, norepinephrine, KCl, vancomycin, verapamil, vit B/C

            Syringe: atropine, heparin

            Y-site: esmolol, heparin

            Not spec: carbenicillin, tetracycline

            IV Incompatibilities

            Additive: amphotericin B

            Syringe: cefazolin, pentobarbital, atropine/pentobarbital, chlorpromazine, heparin (?), secobarbital

            Y-site: allopurinol, amphotericin B, amsacrine, cefepime, indomethacin, warfarin

            IV Preparation

            Solution

            • Injections: in 5% sodium bicarbonate injection, NS, D5W, D10W or LR to a volume of 20 mL
            • Infusions: 300 mg in 100 mL D5W
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            Formulary

            FormularyPatient Discounts

            Adding plans allows you to compare formulary status to other drugs in the same class.

            To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.

            Adding plans allows you to:

            • View the formulary and any restrictions for each plan.
            • Manage and view all your plans together – even plans in different states.
            • Compare formulary status to other drugs in the same class.
            • Access your plan list on any device – mobile or desktop.

            The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
            PA Prior Authorization
            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
            QL Quantity Limits
            Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
            ST Step Therapy
            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
            OR Other Restrictions
            Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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