acetaminophen rectal (OTC)

Brand and Other Names:Acephen, FeverAll, more...FeverAll Infants, FeverAll Junior Strength, Adults' FeverAll
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

suppository

  • 80mg
  • 120mg
  • 325mg
  • 650mg

Antipyretic/Analgesic

325-650 mg PR q4-6hr PRN

Not to exceed 4 g/day

Administration

Patient should lie on left side with knees bent

Remove protective wrap before inserting

Gently insert tip into rectum with slight side-to-side movement (tip of suppository pointing toward navel)

Dosage Forms & Strengths

suppository

  • 80mg
  • 120mg
  • 325mg
  • 650mg

Antipyretic/Analgesic

3 months to 1 year: 80 mg PR q6hr PRN

1-3 years: 80 mg PR q4hr PRN

3-6 years: 120 mg PR q4-6hrPRN

6-12 years: 325 mg PR q4-6hr PRN

>12 years: As adults; 325-650 mg PR q4-6hr PRN

Maximum daily dose

  • <12 years: Not to exceed 5 doses/24 hr
  • ≥12 years: Not to exceed 4 g/day

Administration

Patient should lie on left side with knees bent

Remove protective wrap before inserting

Gently insert tip into rectum with slight side-to-side movement (tip of suppository pointing toward navel)

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Interactions

Interaction Checker

and acetaminophen rectal

No Results

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    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

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             activity indicator 

            Contraindicated (0)

              Serious - Use Alternative (1)

              • lonafarnib

                acetaminophen rectal will increase the level or effect of lonafarnib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration of lonafarnib (a sensitive CYP3A substrate) with weak CYP3A inhibitors is unavoidable, reduce to, or continue lonafarnib at starting dose. Closely monitor for arrhythmias and events (eg, syncope, heart palpitations) since lonafarnib effect on QT interval is unknown.

              Monitor Closely (17)

              • avapritinib

                acetaminophen rectal will increase the level or effect of avapritinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • axitinib

                acetaminophen rectal increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • eltrombopag

                eltrombopag increases levels of acetaminophen rectal by decreasing metabolism. Use Caution/Monitor. UGT inhibition; significance of interaction unclear.

              • finerenone

                acetaminophen rectal will increase the level or effect of finerenone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Monitor serum potassium during initiation and dosage adjustment of either finererone or moderate CYP3A4 inhibitors. Adjust finererone dosage as needed.

              • flibanserin

                acetaminophen rectal will increase the level or effect of flibanserin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Increased flibanserin adverse effects may occur if coadministered with multiple weak CYP3A4 inhibitors.

              • imatinib

                imatinib decreases levels of acetaminophen rectal by decreasing hepatic clearance. Modify Therapy/Monitor Closely. In vitro, imatinib was found to inhibit acetaminophen O-glucuronidation (Ki value of 58.5 micro-M) at therapeutic levels; avoid chronic acetaminophen therapy with imatinib; if occasional acetaminophen administered, do not exceed 1300 mg/day.

              • isavuconazonium sulfate

                acetaminophen rectal will increase the level or effect of isavuconazonium sulfate by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • isoniazid

                isoniazid will increase the level or effect of acetaminophen rectal by affecting hepatic enzyme CYP2E1 metabolism. Use Caution/Monitor.

              • ivacaftor

                acetaminophen rectal increases levels of ivacaftor by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Monitor when coadministered with weak CYP3A4 inhibitors .

              • lemborexant

                acetaminophen rectal will increase the level or effect of lemborexant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Lower nightly dose of lemborexant recommended if coadministered with weak CYP3A4 inhibitors. See drug monograph for specific dosage modification.

              • levonorgestrel oral/ethinylestradiol/ferrous bisglycinate

                levonorgestrel oral/ethinylestradiol/ferrous bisglycinate will decrease the level or effect of acetaminophen rectal by unknown mechanism. Use Caution/Monitor.

              • lomitapide

                acetaminophen rectal increases levels of lomitapide by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Lomitapide dose should not exceed 30 mg/day.

              • midazolam intranasal

                acetaminophen rectal will increase the level or effect of midazolam intranasal by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Coadministration of mild CYP3A4 inhibitors with midazolam intranasal may cause higher midazolam systemic exposure, which may prolong sedation.

              • mipomersen

                mipomersen, acetaminophen rectal. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Both drugs have potential to increase hepatic enzymes; monitor LFTs.

              • tazemetostat

                acetaminophen rectal will increase the level or effect of tazemetostat by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • tetracaine

                tetracaine, acetaminophen rectal. Other (see comment). Use Caution/Monitor. Comment: Monitor for signs of methemoglobinemia when methemoglobin-inducing drugs are coadministered.

              • tinidazole

                acetaminophen rectal will increase the level or effect of tinidazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              Minor (52)

              • acetazolamide

                acetazolamide decreases levels of acetaminophen rectal by increasing metabolism. Minor/Significance Unknown. Enhanced metabolism incr levels of hepatotoxic metabolites.

              • antithrombin alfa

                acetaminophen rectal increases effects of antithrombin alfa by unknown mechanism. Minor/Significance Unknown.

              • antithrombin III

                acetaminophen rectal increases effects of antithrombin III by unknown mechanism. Minor/Significance Unknown.

              • argatroban

                acetaminophen rectal increases effects of argatroban by unknown mechanism. Minor/Significance Unknown.

              • bemiparin

                acetaminophen rectal increases effects of bemiparin by unknown mechanism. Minor/Significance Unknown.

              • bivalirudin

                acetaminophen rectal increases effects of bivalirudin by unknown mechanism. Minor/Significance Unknown.

              • busulfan

                acetaminophen rectal increases levels of busulfan by decreasing metabolism. Minor/Significance Unknown.

              • carbamazepine

                carbamazepine decreases levels of acetaminophen rectal by increasing metabolism. Minor/Significance Unknown. Enhanced metabolism incr levels of hepatotoxic metabolites.

              • cholestyramine

                cholestyramine decreases levels of acetaminophen rectal by inhibition of GI absorption. Applies only to oral form of both agents. Minor/Significance Unknown.

              • clonazepam

                clonazepam decreases levels of acetaminophen rectal by increasing metabolism. Minor/Significance Unknown. Enhanced metabolism incr levels of hepatotoxic metabolites.

              • colestipol

                colestipol decreases levels of acetaminophen rectal by inhibition of GI absorption. Applies only to oral form of both agents. Minor/Significance Unknown.

              • dalteparin

                acetaminophen rectal increases effects of dalteparin by unknown mechanism. Minor/Significance Unknown.

              • diazepam

                diazepam decreases levels of acetaminophen rectal by increasing metabolism. Minor/Significance Unknown. Enhanced metabolism incr levels of hepatotoxic metabolites.

              • disulfiram

                disulfiram will increase the level or effect of acetaminophen rectal by affecting hepatic enzyme CYP2E1 metabolism. Minor/Significance Unknown.

              • enoxaparin

                acetaminophen rectal increases effects of enoxaparin by unknown mechanism. Minor/Significance Unknown.

              • ethanol

                ethanol will decrease the level or effect of acetaminophen rectal by affecting hepatic enzyme CYP2E1 metabolism. Minor/Significance Unknown.

                ethanol increases toxicity of acetaminophen rectal by decreasing metabolism. Minor/Significance Unknown.

              • ethosuximide

                ethosuximide decreases levels of acetaminophen rectal by increasing metabolism. Minor/Significance Unknown. Enhanced metabolism incr levels of hepatotoxic metabolites.

              • exenatide injectable solution

                exenatide injectable solution decreases levels of acetaminophen rectal by unspecified interaction mechanism. Minor/Significance Unknown.

              • exenatide injectable suspension

                exenatide injectable suspension decreases levels of acetaminophen rectal by unspecified interaction mechanism. Minor/Significance Unknown.

              • felbamate

                felbamate decreases levels of acetaminophen rectal by increasing metabolism. Minor/Significance Unknown. Enhanced metabolism incr levels of hepatotoxic metabolites.

              • fondaparinux

                acetaminophen rectal increases effects of fondaparinux by unknown mechanism. Minor/Significance Unknown.

              • fosphenytoin

                fosphenytoin decreases levels of acetaminophen rectal by increasing metabolism. Minor/Significance Unknown. Enhanced metabolism incr levels of hepatotoxic metabolites.

              • gabapentin

                gabapentin decreases levels of acetaminophen rectal by increasing metabolism. Minor/Significance Unknown. Enhanced metabolism incr levels of hepatotoxic metabolites.

              • gabapentin enacarbil

                gabapentin enacarbil decreases levels of acetaminophen rectal by increasing metabolism. Minor/Significance Unknown. Enhanced metabolism incr levels of hepatotoxic metabolites.

              • green tea

                green tea increases effects of acetaminophen rectal by pharmacodynamic synergism. Minor/Significance Unknown. (Theoretical, due to caffeine content).

              • heparin

                acetaminophen rectal increases effects of heparin by unknown mechanism. Minor/Significance Unknown.

              • isoniazid

                isoniazid increases toxicity of acetaminophen rectal by unknown mechanism. Minor/Significance Unknown.

              • lacosamide

                lacosamide decreases levels of acetaminophen rectal by increasing metabolism. Minor/Significance Unknown. Enhanced metabolism incr levels of hepatotoxic metabolites.

              • lamotrigine

                lamotrigine decreases levels of acetaminophen rectal by increasing metabolism. Minor/Significance Unknown. Enhanced metabolism incr levels of hepatotoxic metabolites.

              • levetiracetam

                levetiracetam decreases levels of acetaminophen rectal by increasing metabolism. Minor/Significance Unknown. Enhanced metabolism incr levels of hepatotoxic metabolites.

              • lorazepam

                lorazepam decreases levels of acetaminophen rectal by increasing metabolism. Minor/Significance Unknown. Enhanced metabolism incr levels of hepatotoxic metabolites.

              • methsuximide

                methsuximide decreases levels of acetaminophen rectal by increasing metabolism. Minor/Significance Unknown. Enhanced metabolism incr levels of hepatotoxic metabolites.

              • metoclopramide

                metoclopramide increases levels of acetaminophen rectal by enhancing GI absorption. Applies only to oral form of both agents. Minor/Significance Unknown.

              • metronidazole

                metronidazole will increase the level or effect of acetaminophen rectal by affecting hepatic enzyme CYP2E1 metabolism. Minor/Significance Unknown.

              • oxcarbazepine

                oxcarbazepine decreases levels of acetaminophen rectal by increasing metabolism. Minor/Significance Unknown. Enhanced metabolism incr levels of hepatotoxic metabolites.

              • oxybutynin

                oxybutynin decreases levels of acetaminophen rectal by unspecified interaction mechanism. Minor/Significance Unknown.

              • oxybutynin topical

                oxybutynin topical decreases levels of acetaminophen rectal by unspecified interaction mechanism. Minor/Significance Unknown.

              • oxybutynin transdermal

                oxybutynin transdermal decreases levels of acetaminophen rectal by unspecified interaction mechanism. Minor/Significance Unknown.

              • phenindione

                acetaminophen rectal increases effects of phenindione by unknown mechanism. Minor/Significance Unknown.

              • phenobarbital

                phenobarbital decreases levels of acetaminophen rectal by increasing metabolism. Minor/Significance Unknown. Enhanced metabolism incr levels of hepatotoxic metabolites.

              • phenytoin

                phenytoin decreases levels of acetaminophen rectal by increasing metabolism. Minor/Significance Unknown. Enhanced metabolism incr levels of hepatotoxic metabolites.

              • primidone

                primidone decreases levels of acetaminophen rectal by increasing metabolism. Minor/Significance Unknown. Enhanced metabolism incr levels of hepatotoxic metabolites.

              • protamine

                acetaminophen rectal increases effects of protamine by unknown mechanism. Minor/Significance Unknown.

              • rifabutin

                rifabutin decreases levels of acetaminophen rectal by increasing metabolism. Minor/Significance Unknown. Enhanced metabolism incr levels of hepatotoxic metabolites.

              • rifampin

                rifampin decreases levels of acetaminophen rectal by increasing metabolism. Minor/Significance Unknown. Enhanced metabolism incr levels of hepatotoxic metabolites.

              • rufinamide

                rufinamide decreases levels of acetaminophen rectal by increasing metabolism. Minor/Significance Unknown. Enhanced metabolism incr levels of hepatotoxic metabolites.

              • ruxolitinib

                acetaminophen rectal will increase the level or effect of ruxolitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.

              • tiagabine

                tiagabine decreases levels of acetaminophen rectal by increasing metabolism. Minor/Significance Unknown. Enhanced metabolism incr levels of hepatotoxic metabolites.

              • topiramate

                topiramate decreases levels of acetaminophen rectal by increasing metabolism. Minor/Significance Unknown. Enhanced metabolism incr levels of hepatotoxic metabolites.

              • valproic acid

                valproic acid decreases levels of acetaminophen rectal by increasing metabolism. Minor/Significance Unknown. Enhanced metabolism incr levels of hepatotoxic metabolites.

              • warfarin

                acetaminophen rectal increases effects of warfarin by unknown mechanism. Minor/Significance Unknown.

              • zonisamide

                zonisamide decreases levels of acetaminophen rectal by increasing metabolism. Minor/Significance Unknown. Enhanced metabolism incr levels of hepatotoxic metabolites.

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              Adverse Effects

              Frequency Not Defined

              Pruritic maculopapular rash

              Urticaria

              Rectal discomfort

              Angioedema

              Increase in bilirubin, alkaline phosphatase

              Nephrotoxicity (chronic overdose)

              Analgesic nephropathy

              Decrease in chloride, glucose, uric acid

              Laryngeal edema

              Agranulocytosis

              Decrease in bicarbonate, sodium, calcium

              Leukopenia

              Neutropenia

              Pancytopenia

              Thrombocytopenia

              Thrombocytopenic purpura

              Anaphylactoid reaction

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              Warnings

              Contraindications

              Hypersensitivity

              Cautions

              Acetaminophen is available in many dosage forms and products, check label carefully to avoid overdose

              Risk of hepatotoxicity is higher in alcoholics, chronic high dose, or use of more than one acetaminophen-containing product

              G6PD deficiency

              Risk for rare, but serious skin reactions that can be fatal; these reactions include Stevens-Johnson Syndrome (SJS), toxic epidermal necrolysis (TEN), and acute generalized exanthematous pustulosis (AGEP); symptoms may include skin redness, blisters and rash

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              Pregnancy & Lactation

              Pregnancy category: B; Crosses placenta, safe to use in all stages of pregnancy short term

              Lactation: Excreted in breast milk; compatible w/ breastfeeding

              Pregnant or breastfeeding patients should seek advice of health professional before using OTC drugs

              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.

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              Pharmacology

              Mechanism of Action

              Inhibits prostaglandin synthesis in the CNS and works peripherally to block pain impulse generation; acts on hypothalamus to produce antipyresis

              Pharmacokinetics

              Onset: 1 hr

              Duration: 4-6 hr (analgesia)

              Half-life: 2.4 hr (adolescents); 2-3 hr (adults); 2-5 hr (children); 4-10 hr (neonates)

              Plasma Time: 107-288 min

              Peak Plasma Concentration: dose-dependent; (10 mg/kg) 5.5 mcg/mL, (20 mg/kg) 8.8 mcg/mL, (30 mg/kg) 14.2 mcg/mL

              Protein Bound: 10-25% (therapeutic concentrations); 43% (toxic concentrations)

              Distribution: 1 L/kg

              Metabolism: Liver (microsomal enzyme systems); conjugation (glucuronic/sulfuric acid)

              Metabolites: N-acetyl-p-benzoquinoneimine, N-acetylimidoquinone, NAPQI; further metabolized via conjugation with glutathione

              Excretion: <5% is excreted in the urine as unconjugated (free) acetaminophen and 60-80% as glucuronide metabolites

              Hemodialysis: Yes

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              Images

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              Patient Handout

              A Patient Handout is not currently available for this monograph.
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              Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.