4: D

D

dabigatran

da-big′-a tran

Do not confuse Pradaxa with Plavix.

Category and Schedule

Pregnancy Risk Category: C

Drug Class:

Anticoagulant, thrombin inhibitor

Mechanism of Action

A direct thrombin inhibitor that inhibits coagulation by preventing thrombin-mediated effects and by inhibition of thrombin-induced platelet aggregation.

Therapeutic Effect: Produces anticoagulation.

Uses

Prevention of stroke and systemic embolism in patients with nonvalvular atrial fibrillation

Pharmacokinetics

Rapidly absorbed following oral administration. Peak plasma concentrations reached in 1 hr (2 hr if given with food). 35% plasma protein bound. Dabigatran etexilate is a prodrug, converted to active form by plasma and hepatic esterases. Hepatic glucuronidation to active metabolites. Excreted 80% via urine. Half-life: 12–17 hr; elderly: 14–17 hr; mild-to-moderate renal impairment: 15–18 hr; severe renal impairment: 28 hr.

Indications and Dosages

Nonvalvular Atrial Fibrillation

PO

150 mg twice daily.

Conversion from a parenteral anticoagulant: Initiate dabigatran ≤2 hr prior to the time of the next scheduled dose of the parenteral anticoagulant or at the time of discontinuation for a continuously administered parenteral drug; discontinue parenteral anticoagulant at the time of dabigatran initiation.

Elderly older than 65 yr.

No dosage adjustment required unless renal impairment exists; however, increased risk of bleeding has been observed, particularly in elderly patients with low body weight and/or concomitant renal impairment.

Secondary Prevention of Cardioembolic Stroke or TIA

PO

150 mg twice daily initiated within 1–2 wk after stroke onset or earlier in patients at low bleeding risk.

Do not break, chew, or open capsules, as this will lead to 75% increase in absorption and potentially serious adverse reactions. May be taken without regard to meals.

Side Effects/Adverse Reactions

Frequent

Dyspepsia, abdominal discomfort and pain, bleeding

Occasional

GERD, esophagitis, anemia, hematuria, hematoma, epistaxis, wound secretion, anaphylaxis

Precautions and Contraindications

Hypersensitivity to dabigatran or any component of the formulation. May cause fatal bleeding. No specific antidote exists for dabigatran reversal; protamine and vitamin K do not reverse or impact anticoagulant effects of dabigatran. Use in patients with severe renal and hepatic impairment and valvular heart disease is not recommended. Use with extreme caution in elderly patients. Avoid use in patients taking other anticoagulants and P-glycoprotein inducers/inhibitors.

Drug Interactions of Concern to Dentistry

• Increased risk of bleeding: NSAIDs, aspirin

• P-gp inducers (e.g., carbamazepine, barbiturates, St. John’s wort): reduced blood levels and effectiveness of dabigatran

• P-gp inhibitors and CYP3A4 inhibitors (e.g., macrolide antibiotics, azole antifungals): increased blood levels and adverse effects of dabigatran

Serious Reactions

! Discontinuing dabigatran, for elective and/or invasive procedures, increases the risk of stroke, which is sometimes fatal.

Dental Considerations

General:

• Increased intra- and postoperative bleeding, additional hemostatic measures are indicated.

• Monitor vital signs at every visit due to existing cardiovascular disease.

• Avoid discontinuation of drug therapy for routine dental procedures without consulting patient’s prescribing physician.

Consultations:

• Consult physician to determine patient’s coagulation status and risk for complications.

Teach Patient/Family to:

• Report changes in drug regimen.

• Report signs and symptoms of excessive postoperative bleeding.

daclizumab

day-cly′-zu-mab

Category and Schedule

Pregnancy Risk Category: C

Drug Class:

Immunosuppressive, IgG1 monoclonal antibody

Mechanism of Action

A monoclonal antibody that binds to the interleukin-2 (IL-2) receptor complex, inhibiting the IL-2-mediated activation of T lymphocytes, a critical pathway in the cellular immune response involved in allograft rejection.

Therapeutic Effect: Prevents organ rejection.

Uses

Prophylaxis of acute organ rejection in patients with renal transplants; used in combination with cyclosporine and glucocorticoids.

Pharmacokinetics

Half-life: Adults, 20 days.

Indications and Dosages

Prevention of Acute Renal Transplant Rejection (in combination with an immunosuppressive)

IV

Adults, Children.

1 mg/kg over 15 min q14 days for 5 doses, beginning no more than 24 hr before transplantation. Maximum: 100 mg.

Side Effects/Adverse Reactions

Occasional

Constipation, nausea, diarrhea, vomiting, abdominal pain, edema, headache, dizziness, fever, pain, fatigue, insomnia, weakness, arthralgia, myalgia, diaphoresis

Precautions and Contraindications

Caution:

Risk of lymphoproliferative disease and opportunistic infections, anaphylaxis risk unknown, long-term effects unknown, lactation, children, geriatric patients

Drug Interactions of Concern to Dentistry

• None reported

Serious Reactions

! Hypersensitivity reaction, which occurs rarely, is characterized by dyspnea, tachycardia, dysphagia, peripheral edema, rash, and pruritus.

Dental Considerations

General:

• This is a hospital-type drug, but because some dosing is continued, patients may appear in the dental office while receiving this drug.

• Transplant patients may also be taking cyclosporine and glucocorticoids; review each transplant patient’s medications.

• Short appointments and a reduction protocol may be required for anxious patients.

Consultations:

• Antibiotic prophylaxis usually is recommended in patients with organ transplants and immunosuppression.

• Medical consultation may be required to assess disease control and patient’s ability to tolerate stress.

Teach Patient/Family to:

• Encourage effective oral hygiene to prevent soft tissue inflammation.

• Prevent trauma when using oral hygiene aids.

• Update health and drug history if physician makes any changes in evaluation or drug regimens.

dalfampridine

dal-fam-pri-deen

Category and Schedule

Pregnancy Risk Category: C

Drug Class:

Potassium channel blocker

Mechanism of Action

A potassium channel blocker that increases conduction of action potentials in demyelinated axons.

Therapeutic Effect: Improved walking speed.

Uses

Multiple sclerosis

Pharmacokinetics

Rapidly and completely absorbed after PO administration. Unbound to plasma proteins. Well distributed in saliva. Minimally metabolized in liver. Primarily excreted unchanged (90%) in urine. CYP2E1 is the major isoenzyme responsible for the 3-hydroxylation of dalfampridine. Half-life: 5.2–6.5 hr.

Indications and Dosages

Multiple Sclerosis

PO

Adults.

10 mg twice a day, 12 hr apart. Max: 20 mg/day.

Side Effects/Adverse Reactions

Frequent

Nausea, vomiting, urinary tract infection

Occasional

Abdominal pain, abnormal gait, backache, asthenia, dizziness, headache, insomnia, anxiety

Rare

Constipation, indigestion, multiple sclerosis relapse, paresthesia, seizure, nasopharyngitis, pain in throat

Precautions and Contraindications

Hypersensitivity to dalfampridine or its components

Renal impairment, moderate or severe (CrCl ≤ 50 mL/min)

History of seizures

Caution:

Concomitant use with 4-aminopyridine derivatives

Mild renal impairment

Drug Interactions of Concern to Dentistry

• None reported

Serious Reactions

! Seizures have been observed and appear to be dose related.

Dental Considerations

General:

• Consider semisupine chair position for patient comfort if GI side effects occur.

Consultations:

• Medical consultation may be required to assess disease control.

Teach Patient/Family to:

• Encourage effective oral hygiene to prevent soft tissue inflammation.

• Prevent trauma when using oral hygiene aids.

• Be alert for the possibility of secondary oral infection and the need to see dentist immediately if signs of infection occur.

dalteparin sodium

doll′-teh-pare-in so′-dee-um

Category and Schedule

Pregnancy Risk Category: B

Drug Class:

Heparin-type anticoagulant

Mechanism of Action

An antithrombin that inhibits factor Xa and thrombin in the presence of low-molecular-weight heparin. Only slightly influences platelet aggregation, PT, and aPTT.

Therapeutic Effect: Produces anticoagulation.

Uses

Prevention of deep vein thrombosis (DVT) following abdominal surgery, treatment of life-threatening conditions such as unstable angina, non–Q-wave MI; prevention of ischemia complications caused by blood clot formation in patients on aspirin therapy; in combination with warfarin in deep vein thrombosis with or without pulmonary embolism (PE)

Pharmacokinetics

Protein binding: less than 10%. Half-life: 3–5 hr.

Indications and Dosages

Low- to Moderate-Risk Abdominal Surgery

Subcutaneous

Adults, Elderly.

2500 international units 1–2 hr before surgery, then daily for 5–10 days.

High-Risk Abdominal Surgery

Subcutaneous

Adults, Elderly.

5000 international units 1–2 hr before surgery, then daily for 5–10 days.

Total Hip Surgery

Subcutaneous

Adults, Elderly.

2500 international units 1–2 hr before surgery, then 2500 units 6 hr after surgery, then 5000 units/day for 7–10 days.

Unstable Angina, Non–Q-Wave MI

Subcutaneous

Adults, Elderly.

120 international units/kg q12h (maximum: 10,000 international units/dose) given with aspirin until clinically stable.

Prevention of DVT or PE in the Acutely Ill Patient

Subcutaneous

Adults, Elderly.

5000 international units once a day.

Side Effects/Adverse Reactions

Occasional

Hematoma at injection site

Rare

Hypersensitivity reaction (chills, fever, pruritus, urticaria, asthma, rhinitis, lacrimation, headache); mild, local skin irritation

Precautions and Contraindications

Active major bleeding; concurrent heparin therapy; hypersensitivity to dalteparin, heparin, or pork products; thrombocytopenia associated with positive in vitro test for antiplatelet antibody

Caution:

Hemorrhage, cannot be used interchangeably with other forms of heparin, lactation, children, requires monitoring, GI bleeding

Drug Interactions of Concern to Dentistry

• Avoid concurrent use of aspirin (except as noted), NSAIDs, dipyridamole, and sulfinpyrazone.

Serious Reactions

! Overdose may lead to bleeding complications ranging from local ecchymoses to major hemorrhage.

! Thrombocytopenia occurs rarely.

Dental Considerations

General:

• Product may be used in outpatient therapy. Delay elective dental treatment until patient completes anticoagulant therapy; do not discontinue dalteparin.

• Determine why patient is taking the drug.

• Consider local hemostasis measures to prevent excessive bleeding.

• Avoid prescribing aspirin-containing products.

Consultations:

• Medical consultation should include routine blood counts, including platelet counts and aggegration tests.

Teach Patient/Family to:

• Encourage effective oral hygiene to prevent soft tissue inflammation.

• Prevent trauma when using oral hygiene aids.

• Report oral lesions, soreness, or bleeding to dentist.

danaparoid

da-nah′-pah-roid

Category and Schedule

Pregnancy Risk Category: B

Drug Class:

Heparinoid-type anticoagulant

Mechanism of Action

An antithrombotic agent that inhibits thrombin formation through factor antiXa and antiIIa effects. Does not significantly influence bleeding time, PT, aPTT, or platelet function. Possesses greater antithrombotic activity than anticoagulant activity.

Uses

Prevention of deep vein thrombosis (DVT) following hip or knee replacement surgery; unapproved: thromboembolism, hemodialysis, and cardiovascular surgery

Pharmacokinetics

Well absorbed following subcutaneous administration. Eliminated primarily in the urine. Half-life: 24 hr (half-life prolonged with severe renal impairment).

Indications and Dosages

Note: Give initial dose as soon as possible after surgery but not more than 24 hr after surgery.

Prevention of DVT

Subcutaneous

Adults, Elderly.

750 anti-Xa units twice daily beginning 1–4 hr preoperatively and then not sooner than 2 hr after surgery. Continue treatment throughout postoperative care until risk of DVT has diminished (average duration 7–14 days).

Side Effects/Adverse Reactions

Frequent

Injection site pain

Occasional

Fever, pain, nausea, UTI, constipation

Rare

Rash, pruritus, infection

Precautions and Contraindications

Severe hemorrhagic diathesis (hemophilia, idiopathic thrombocytopenic purpura), active major bleeding state, including hemorrhagic stroke in the acute phase, type II phase thrombocytopenia associated with positive in vitro test for antiplatelet antibody in presence of danaparoid, hypersensitivity to pork products, danaparoid, or any component of the formulation

Caution:

Cannot interchange with heparin, hemorrhage, thrombocytopenia, renal or hepatic impairment, lactation, children, antidotes not available, GI bleeding

Drug Interactions of Concern to Dentistry

• Avoid concurrent use of platelet aggregation antagonist, such as aspirin; NSAIDs; dipyridamole.

Serious Reactions

! Accidental overdosage may lead to bleeding complications ranging from minor ecchymosis to major hemorrhage. An unexplained fall in HCT or fall in B/P should lead to consideration of a hemorrhagic event. The antidote protamine sulfate only partially neutralizes danaparoid activity and is incapable of reducing severe nonsurgical bleeding during treatment. If serious bleeding occurs, discontinue danaparoid; give blood or blood product transfusions.

Dental Considerations

General:

• Determine why patient is taking the drug.

• Do not discontinue danaparoid.

• Consider local hemostasis measures to prevent excessive bleeding if dental treatment must be performed.

• Delay elective dental treatment until patient completes danaparoid therapy.

Consultations:

• Medical consultation should include routine blood counts, including platelet counts and bleeding time.

Teach Patient/Family to:

• Encourage effective oral hygiene to prevent soft tissue inflammation.

• Use caution to prevent trauma when using oral hygiene aids.

• Report oral lesions, soreness, or bleeding to dentist.

danazol

(Cyclomen[can], Danocrine)

Category and Schedule

Pregnancy Risk Category: X

Drug Class:

Androgen, α-ethinyl testosterone derivative

Mechanism of Action

A testosterone derivative that suppresses the pituitary-ovarian axis by inhibiting the output of pituitary gonadotropins. Causes atrophy of both normal and ectopic endometrial tissue in endometriosis. Follicle-stimulating hormone (FSH) and luteinizing hormone (LH) are depressed in fibrocystic breast disease. Inhibits steroid synthesis and binding of steroids to their receptors in breast tissues. Increases serum levels of esterase inhibitor.

Therapeutic Effect: Produces anovulation and amenorrhea, reduces the production of estrogen, corrects biochemical deficiency as seen in hereditary angioedema.

Uses

Treatment of endometriosis, prevention of hereditary angioedema, fibrocystic breast disease

Pharmacokinetics

Well absorbed from GI tract. Metabolized in liver, primarily to 2-hydroxymethylethisterone. Excreted in urine. Half-life: 4.5 hr.

Indications and Dosages

Endometriosis

PO

Adults.

200–800 mg/day in 2 divided doses for 3–9 mo.

Fibrocystic Breast Disease

PO

Adults.

100–400 mg/day in 2 divided doses.

Hereditary Angioedema

PO

Adults.

Initially, 200 mg 2–3 times a day. Decrease dose by 50% or less at 1–3 mo intervals. If attack occurs, increase dose by up to 200 mg/day.

Side Effects/Adverse Reactions

Frequent

Females: Amenorrhea, breakthrough bleeding/spotting, decreased breast size, increased weight, irregular menstrual period.

Occasional

Males/females: Edema, rhabdomyolysis (muscle cramps, unusual fatigue), virilism (acne, oily skin), flushed skin, altered moods

Example: Danazol (generic name), 100 mg

Rare

Males/females: Hematuria, gingivitis, carpal tunnel syndrome, cataracts, severe headache, vomiting, rash, photosensitivity

Females: Enlarged clitoris, hoarseness, deepening voice, hair growth, monilial vaginitis

Males: Decreased testicle size

Precautions and Contraindications

Cardiac impairment, hypercalcemia, pregnancy, prostatic or breast cancer in males, severe liver or renal disease

Caution:

Migraine headaches, seizure disorders

Drug Interactions of Concern to Dentistry

• Increased serum concentration of carbamazepine; consider avoiding concurrent administration.

Serious Reactions

! Jaundice may occur in those receiving 400 mg/day or more. Liver dysfunction, eosinophilia, thrombocytopenia, pancreatitis occur rarely.

Dental Considerations

General:

• Patients on chronic drug therapy may rarely have symptoms of blood dyscrasias, which can include infection, bleeding, and poor healing.

Consultations:

• In a patient with symptoms of blood dyscrasias, request a medical consultation for blood studies and postpone dental treatment until normal values are reestablished.

Teach Patient/Family to:

• Encourage effective oral hygiene to prevent soft tissue inflammation.

• Avoid mouth rinses with high alcohol content because of drying and irritating effects.

dantrolene sodium

dan′-troe-leen so′-dee-um

Do not confuse Dantrium with Daraprim.

Category and Schedule

Pregnancy Risk Category: C

Drug Class:

Skeletal muscle relaxant, direct-acting

Mechanism of Action

A skeletal muscle relaxant that reduces muscle contraction by interfering with release of calcium ion. Reduces calcium ion concentration.

Therapeutic Effect: Dissociates excitation-contraction coupling. Interferes with catabolic process associated with malignant hyperthermic crisis.

Uses

Treatment of spasticity in multiple sclerosis, stroke, spinal cord injury, cerebral palsy, malignant hyperthermia

Pharmacokinetics

Poorly absorbed from the GI tract. Protein binding: High. Metabolized in the liver. Primarily excreted in urine. Half-life: IV: 4–8 hr; PO: 8.7 hr.

Indications and Dosages

Spasticity

PO

Adults, Elderly.

Initially, 25 mg/day. Increase to 25 mg 2–4 times a day, then by 25-mg increments up to 100 mg 2–4 times a day.

Children.

Initially, 0.5 mg/kg twice a day. Increase to 0.5 mg/kg 3–4 times a day, then in increments of 0.5 mg/kg/day up to 3 mg/kg 2–4 times a day. Maximum: 400 mg/day.

Prevention of Malignant Hyperthermic Crisis

PO

Adults, Elderly, Children.

4–8 mg/kg/day in 3–4 divided doses 1–2 days before surgery; give last dose 3–4 hr before surgery.

IV

Adults, Elderly, Children.

2.5 mg/kg about 1.25 hr before surgery.

Management of Malignant Hyperthermic Crisis

IV

Adults, Elderly, Children.

Initially, a minimum of 1 mg/kg rapid IV; may repeat up to total cumulative dose of 10 mg/kg. May follow with 4–8 mg/kg/day PO in 4 divided doses up to 3 days after crisis.

Side Effects/Adverse Reactions

Frequent

Drowsiness, dizziness, weakness, general malaise, diarrhea (mild)

Occasional

Confusion, diarrhea (may be severe), headache, insomnia, constipation, urinary frequency

Rare

Paradoxical CNS excitement or restlessness, paresthesia, tinnitus, slurred speech, tremors, blurred vision, dry mouth, nocturia, impotence, rash, pruritus

Precautions and Contraindications

Active hepatic disease

Caution:

Peptic ulcer disease, renal disease, hepatic disease, stroke, seizure disorder, diabetes mellitus, elderly; monitor liver enzymes

Drug Interactions of Concern to Dentistry

• None reported

Serious Reactions

! There is a risk of liver toxicity, most notably in females, those 35 yr of age and older, and those taking other medications concurrently.

! Overt hepatitis noted most frequently between 3rd and 12th mo of therapy.

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Tags: Mosbys Dental Drug Reference 11e

Jan 5, 2015 | Posted by mrzezo in General Dentistry | Comments Off

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