Pathopharm Final Exam Medications

Naloxone

• Competitive antagonist

• Reversal of opioid overdose

  • Drug of choice with pure opioid agonist overdose

  • Titrated cautiously with physical dependence

• Reversal of postoperative opioid effects

  • Titrated to achieve adequate ventilation and to maintain pain relief

• Reversal of neonatal respiratory depression

• Opioids given during labor and delivery may cause respiratory depression in neonate

Ketorolac

• NSAID

• Opioid-like effects

• Avoid during pregnancy

• Oral, IM, IV, opthalmic

• SHORT TERM USE

  • 5 days max

    • Increased risk of thrombotic events if used >5 days

NSAIDS

• Examples: aspirin, ibuprofen, naproxen

• Pain relief, suppression of inflammation, and reduction of fever

• Adverse effects: gastric ulceration, acute renal failure, and bleeding

• All except aspirin increase the risk of thrombotic events (e.g., myocardial infarction, stroke)

• Do not cause tolerance, physical dependence, or psychologic dependence

Acetaminophen

• Non-opioid analgesic

• Tylenol

• Inhibit COX in the central nervous system but not in the periphery

• Combining acetaminophen with an opioid can produce greater analgesia than either drug alone

  • Norco/Lortab (hydrocode-acetaminophen)

  • Percocet (Oxycodone-acetaminophen)

• Lacks anti-inflammatory actions

• Does not inhibit platelet aggregation

• Does not promote gastric ulceration, renal failure, or thrombotic events

• Caution in patients with liver problems

Disulfiram

• Drug used to maintain abstinence

• Refrain from drinking

• Causes irreversible inhibition of aldehyde dehydrogenase

• Effects caused by alcohol plus disulfiram are referred to as acetaldehyde syndrome

• Patients must be carefully chosen

• Patients must be thoroughly informed to avoid all forms of alcohol, including the following:

  • Sauces

  • Cough syrups

  • Alcohol applied to the skin (eg, lotions, colognes, liniments)

Lidocaine w/ epinephrine

• Local anesthetic

• Epinephrine may be added

  • Vasoconstricts; keeps medication local to prevent systemic effects

  • Increases duration of Lidocaine effects

  • Not for areas with small capillaries

N-acetylcysteine

• Acetaminophen antidote

• Tastes terrible (may need to administer in soda or other flavored beverage)

Methadone

• Strong opioid agonist

• Long-term opioid addication management, maintence and suppressive therapy

• Treatment for pain and opioid addicts

Bupropion

• Atypical antidepressant

• Reduces the urge to smoke and reduces some symptoms of nicotine withdrawal, such as irritability and anxiety

• Adverse effects: dry mouth and insomnia

Kava

• Used for relaxation and anxiety

• Can result in severe hepatic damage

St. John’s Wort

• Limited clinical studies show that St. John’s wort is useful for mild to moderate depression, not for severe depression

• No prescription needed in the United States

• Decrease reuptake of serotonin, norepinephrine, and dopamine

• Interacts adversely with many drugs

  • Induction of cytochrome P450 enzymes

  • Induction of P-glycoprotein

  • Intensification of serotonin effect (serotonin syndrome in antidepressants)

  • Warfarin

  • Decreases effectiveness of birth control

Diphenhydramine

• Antihistamine

• Use

  • Allergic rhinitis, pruritus, urticaria

  • Common cold, sneezing, cough

  • Prevent motion sickness

  • Promote sleep

• Contraindications/cautions

  • Closed-angle glaucoma, urinary retention

  • Severe liver disease

• Interactions

  • Increases CNS depression with alcohol and other CNS depressants

Diphenhydramine - take action

• Give oral form of diphenhydramine with food to decrease gastric distress

• Warn the patient to avoid driving a motor vehicle and performing dangerous activities until stabilized on the drug

• Advise the patient to avoid alcohol and other CNS depressants

• Suggest use of sugarless candy, gum, or ice chips for relief of mouth dryness

• Evaluate outcomes

Albuterol

• Bronchodilator

• Rapid onset of action

• Longer duration of action

• Few side effects

• Use

  • Asthma, acute bronchospasm

  • Bronchospasm prophylaxis

• Common side effects

  • Headache, rhinitis, excitability, tremors

  • Bronchospasm, palpitations, tachycardia

Salmeterol

• Bronchodilator

• Long-acting Beta2 agonist

• Uses

  • Long-term maintenance of asthma

  • Prevention exercise-induced asthma

  • COPD

• Inhaled

• Adverse reactions

  • Anxiety, H/A, nervousness, sleep disturbance

  • Tachycardia, HTN

  • Oral candidiasis

Pseudoephedrine

• Nasal decongestant

• Sudafed

• Less stimulating

• Controlled d/t methamphetamine production

Tiotropium

• Bronchodilator

• Use

  • Maintenance treatment of bronchospasms associated with COPD

• Administered by inhalation only with the HandiHaler device (dry-powder capsule inhaler)

• Common side effects

  • Dry mouth, constipation, GI distress

  • Depression, insomnia, headache

  • Pharyngitis, sinusitis, infection

  • Arthralgia, peripheral edema

Prednisone

• Steroid

• Preferred drug for oral therapy of chronic adrenal insufficiency

• Cortisone is a prodrug that undergoes conversion to hydrocortisone (its active form) in the body; the drug has both glucocorticoid and mineralocorticoid activity

Hydrocortisone

• Glucorticoid

• Synthetic steroid with a structure identical to that of cortisol

• Drug for inflammatory bowel disease

• Therapeutic uses

  • Adrenal insufficiency

  • Allergic reactions to inflammation

  • Cancer

• Adverse effects of high-dose therapy

  • Adrenal suppression

  • Cushing’s syndrome

Insulin glargine

• Long-duration insulin

• Modified human insulin

• Prolonged duration of action (up to 24 hours)

• Once-daily subQ dosing to treat adults and children with type 1 diabetes and adults with type 2 diabetes

• Clear solution

Regular insulin

• Short-acting insulin

• Unmodified human insulin

• Four approved routes: SubQ injection, subQ infusion, intramuscular (IM) injection (used rarely), and oral inhalation (approved but not currently used)

• Effects begin in 30 to 60 minutes

• Peak in 1 to 5 hours

• Duration up to 10 hours

• Clear solution

NPH insulin

• Intermediate-duration insulin

• Drug is injected twice or 3 times daily to provide glycemic control between meals and during the night

• NPH insulin is the only one suitable for mixing with short-acting insulins

• Allergic reactions are possible

• NPH insulins are cloudy suspensions that must be agitated before administration

• NPH insulins are administered by subQ injection only

Tamsulosin

• Urinary retention medication

• Flomax

• Used to treat symptomatic benign prostatic hyperplasia and chronic prostatitis and to help with the passage of kidney stones

• It works by relaxing the muscles in the prostate and bladder so that urine can flow easily

• Tamsulosin may cause a sudden drop in your blood pressure, which could lead to dizziness or fainting, this risk is higher when you first start taking this drug

Cimetidine

• Histamine2 receptor antagonist

• First-choice drug for treating gastric and duodenal ulcers

• Promote healing by suppressing secretion of gastric acid

• Pharmacokinetics

  • Absorption is slowed if taken with meals

  • Crosses the blood-brain barrier with difficulty

  • May cause some CNS side effects

• Adverse effects

  • Antiandrogenic effects

  • CNS effects

  • Pneumonia

  • IV bolus: Can cause hypotension and dysrhythmias

• Drug interactions

  • Warfarin, phenytoin, theophylline, lidocaine

  • Antacids can reduce absorption of cimetidine

  • Cimetidine and antacids should be administered at least 1 hour apart

Pantoprazole

• Similar to omeprazole and the other PPIs

• Uses: treatment of GERD and hypersecretory states

• Adverse effects

  • Oral: diarrhea, headache, dizziness

  • IV: diarrhea, headache, nausea, dyspepsia, injection-site reactions, including thrombophlebitis and abscess

  • Long-term use: hypomagnesemia, osteoporosis, fractures

Omeprazole

• First available PPI

• Actions and characteristics

  • Inhibits gastric secretion

  • Short half-life

  • Used for short-term therapy

  • Ulcer prophylaxis is indicated only for patients in intensive care units, and then only if they have an additional risk factor, such as multiple trauma, spinal cord injury, or prolonged mechanical ventilation (longer then 48 hours)

• Adverse effects

  • Usually inconsequential with short-term use

  • Headache

  • GI effects

  • Pneumonia

  • Fractures

  • Hypomagnesemia

  • Rebound acid hypersecretion

  • C. difficile infection

  • Gastric cancer

Sucralfate

• Antacid

• Treatment of ulcers

• Creates a protective barrier for up to 6 hours

  • Like a bandaid for GI

• Therapeutic uses

  • Acute ulcers and maintenance therapy

• Adverse effects

  • Constipation (only 2% of patients)

• Drug interactions

  • Minimal

  • Antacids may interfere with effects of sucralfate

  • May inhibit absorption of other medications administered simultaneously

    • Give 2 HOURS BEFORE OR AFTER OTHER MEDICATIONS

Dronabinol

• Cannabinoid

• Antiemetic

• Potential for abuse and psychotomimetic effects

• Useful in chemotherapy patients to decrease emesis and stimulate hunger

Levothyroxine

• Synthetic T4

• Hypothyroidism treatment in adults

• Oral: 30-60min before breakfast (empty stomach)

• Typically life-long replacement therapy

• Adverse effects

  • Chest pain, arrhythmias

  • Headache

  • Tremors, nervousness, trouble sleeping

• Careful of refills: not all levothyroxine preparations have the same bioavailability (do not change manufacturer)

Methimazole

• First-line drug for hyperthyroidism

• Prototype of the thionamides

• Does not cause the liver damage associated with propylthiouracil (PTU)

• Does not destroy existing stores of thyroid hormone

• May take 3 to 12 weeks for euthyroid state

• More dangerous than PTU during lactation and during the first trimester of pregnancy

• Agranulocytosis

  • Severe reduction in the number of white blood cells (granulocytes) in the circulating blood

Metformin

• Biguanide

  • Oral hypoglycemic

  • Reduce glucose production in the liver, improve the body’s sensitivity to insulin

• Drug of choice for initial therapy in most patients with type 2 diabetes

• Most common side effects: gastrointestinal (GI) disturbances

• Lactic acidosis, a potentially fatal complication, is rare

  • Do not administer within 48 hours after use of contrast dye

• Prevention of type 2 diabetes

• Gestational diabetes

Lactulose

• Synthetic sugar used to treat constipation

• Treatment of:

  • Chronic constipation

  • Hepatic encephalopathy

• Common side effects

  • Bloating, gas, diarrhea, nausea, vomiting

• Decreases intestinal production and absorption of ammonia

Lorazepam

• Benzodiazepine

• Terminate seizures from generalized convulsive status epilepticus

  • Benzodiazepine lorazepam is recommended for first-line management

  • Diazepam, which is also a benzodiazepine, may be used if lorazepam is not readily available

Alprazolam

• Benzodiazepine (anti-anxiety medication)

• Short acting

• Xanax

Lithium

• Mood stabilizer

  • Relieve symptoms during manic and depressive episodes

  • Prevent recurrence of manic and depressive episodes

  • Do not worsen symptoms of mania or depression; do not accelerate the rate of cycling

Lithium pharmacokinetics

• Short half-life

• Excreted by the kidneys

  • Excretion reduced when serum sodium level low

  • Careful in patients with kidney disfunction

Lithium side effects

• Gastrointestinal upset

• Fine hand tremors

• Polyuria

  • Increased urine decreases levels of sodium and increases level of Lithium, risk of toxicity

• Muscle weakness

• Renal toxicity

• Goiter and hypothyroidism

• Teratogenic

Lithium drug interactions

• Diuretics

  • Sodium loss can increase risk of Lithium toxicity

• Nonsteroidal anti-inflammatory drugs

  • Can increase Lithium levels 60%

• Anticholinergic drugs

  • Anticholinergic urinary hesitancy coupled with Lithium-induced polyuria can result in patient discomfort

Olanzapine

• Atypical antipsychotic agent (second generation)

• Suppresses agitation in severe mania

• Suppresses nausea in chemotherapy

• Schizophrenia treatment

Aripiprazole

• Dopamine system stabilizer

• Treats mania, depression and irritability

• Does not block cholinergic receptors

• Less risk of cardiac arrhythmias

• Low risk of orthostatic hypotension

• Most common side effects are headache, anxiety, and insomnia

Haloperidol

• High potency first generation antipsychotic agent

• Block dopamine receptors in the mesolimbic area of the brain

• Schizophrenia treatment

Carbidopa-levodopa

• Levodopa

  • Dopamine replacement agent for the treatment of PD

  • Only given in combination with carbidopa

  • Highly effective, but benefits diminish over time

• Carbidopa

  • Inhibits peripheral dopamine breakdown

Carbidopa-levodopa advantages

• No adverse effects of its own

• Increases available levodopa in the CNS and allows for 75% decrease in levodopa dosage; therefore, reduces cardiovascular and GI adverse effects (prevents breakdown of levodopa in the periphery, allowing more to reach the brain)

Phenytoin

• Traditional AED

• Partial and tonic-clonic seizures

• Mechanism of action: selective inhibition of sodium channels

• Varied oral absorption

• Half-life: 8 to 60 hours

• Therapeutic levels: 10 to 20 mcg/mL

Phenytoin adverse effects

• Nystagmus

• Sedation

• Ataxia

• Diplopia

• Cognitive impairment

• Gingival hyperplasia: swelling, tenderness, and bleeding of the gums

  • Gingivectomy

    • Surgical procedure that involves removing excess or diseased gum tissue (gingiva) from around the teeth

  • Folic acid (0.5 mg/day) may prevent gum overgrowth

  • Risk can be minimized by good oral hygiene, including dental flossing and gum massage

• Skin rash

• Effects in pregnancy

• Cardiovascular effects

Phenytoin drug interactions

• Decreases the effects of oral contraceptives, warfarin, and glucocorticoids

• Increases levels of diazepam, isoniazid, cimetidine, alcohol, and valproic acid

• Dosing: highly individualized

• Administration: with food

Sertraline

Selective serotonin reuptake inhibitor (SSRI)

Diazepam

• Benzodiazepine

  • The only drug labeled to treat spasm and spasticity

• Mechanism of action

  • Acts in CNS

  • Mimics action of GABA

• Adverse effects

  • CNS depression (sedation)

  • Dependence

    • Withdrawn slowly

Pregabalin

• Analog of GABA

• Neuropathic pain associated with diabetic neuropathy

• Postherpetic neuralgia

• Adjunctive therapy of partial seizures

• Fibromyalgia

• Abuse potential

  • Euphoric effects

  • Schedule V

Pregabalin adverse effects

• Adverse effects: Dizziness, somnolence, blurred vision, significant weight gain, difficulty thinking, headache, peripheral edema, and dry mouth

• Hypersensitivity reactions: life-threatening angioedema

• Rhabdomyolysis

  • Monitor kidney function (BUN and creatinine)

Fluticasone

• Intranasal glucocorticoid medication

• Reduces inflammation and relieves symptoms of various conditions like allergic rhinitis, asthma, and skin conditions

Gabapentin

• Anticonvulsant

• Therapeutic use: adjunctive therapy of partial seizures

• Off-label use: neuropathic pain, prophylaxis of migraine, treatment of fibromyalgia, and relief of postmenopausal hot flashes

Gabapentin adverse reactions

• Very well tolerated

• Most common side effects: somnolence, dizziness, ataxia, fatigue, nystagmus, and peripheral edema

  • Fatigue = has become a drug for abuse

Testosterone

• Androgen

• Maturation of sperm, sex characteristics, protein metabolism, muscle development

Estrogen

Sex hormone responsible for the development and regulation of the female reproductive system and secondary sex characteristics

Venlafaxine

• Serotonin/norepinephrine reuptake inhibitor (SNRIs)

• Effexor

• Indications

  • Major depression

  • Generalized anxiety disorder

  • Social anxiety disorder (social phobia)

  • Panic disorder

• Blocks norepinephrine and serotonin uptake

• Serious reactions if combined with MAOIs

• Therapeutic effect develops over 2-4 weeks

Fluoxetine

• Selective serotonin reuptake inhibitor (SSRIs)

• Antidepressant

• Prozac

• Well absorbed orally – may be taken with food

• Therapeutic effect develops over 2-4 weeks

• Other uses

  • Obsessive-compulsive disorder

  • Bulimia nervosa

  • Premenstrual dysphoric disorder

• Death by overdose is extremely rare

Isoniazid

• Antibiotic

• Used to treat tuberculosis (TB) or prevent its return (reactivation)

• Take with pyridoxine (vitamin B6)

• Avoid foods and drinks high in tyramine or histamine

• Causes urine, stool, saliva, sputum, sweat, teeth, and tears to turn reddish-orange to reddish-brown

Rifampin

• Antibiotic

• Used together with other medicines to treat tuberculosis (TB) by killing meningitis bacteria

Cyclophosphamide

• Alkylating agent

• Cytotoxic medication

• Cell cycle phase nonspecific b/c reactions can take place at anytime

• Cell kill results from alkylation of DNA

Cisplatin

• Platinum compound

• Cytotoxic medication

• Cell cycle phase nonspecific, cross links DNA

Antimetabolites

• Cytotoxic medications

• Folic acid analogs

  • Methotrexate: S-phase specific - disrupts DNA synthesis

• Pyrimidine analogs

  • Fluorouracil: S-phase specific - inhibits DNA and RNA synthesis (kills dividing cells only)

Vincristine

• Miotic inhibitor

• Cytotoxic medication

• Inhibits microtubule formation, stopping mitosis in metaphase

Tamoxifen

• Used for anti-estrogen breast cancer

• Block estrogen receptors

• Used for established breast cancer disease and for reducing occurrence in high-risk patients

• Osteoporosis treatment

• Effects resemble those of estrogen

• Reduces bone resorption and turnover

Leuoprolide

• Leupron

• Hormonal treatment

• Inhibits gonadotropin release, suppressing ovarian and testicular steroidogenesis

Glucosamine/Chondroitin

• Naturally occuring

• Not approved by the FDA for any medical use

• May interact with warfarin to increase bleeding

Glucosamine

Sugar protein that helps the body build cartilage

Chondroitin

Believed to help the body maintain fluid and flexibility in the joints

Aspirin

• First NSAID

• Mild to moderate pain and inflammation

• Decreases platelet aggregation

  • Bleeding risk

• Gastric irritation

  • Risk for ulcer formation

• Tinitis, Headache

  • Salacylate levels

Celecoxib

• NSAID – Cox-2 inhibitor

• Used to treat pain and inflammation related to

  • Arthritis

  • Ankylosing spondylitis

• Increased risk for MI or Stroke (with or without risk factors)

• Stomach or intestinal bleeding

Ibuprofen

• NSAID

• Inhibits cyclooxygenase

• Antinflammatory, analgesic, and antipyretic

• Uses

  • Mild fever

  • Mild to moderate pain

  • Arthritis

• Well tolerated

• Less gastric bleeding than aspirin (less platelet aggregation)

• Increased risk of MI or stroke

Diclofenac sodium

• NSAID

• High first-pass effect

• Highly protein bound

• Topical use is most common (now OTC)

• Uses: Anti-inflammatory, analgesic, antipyretic

  • Osteoarthritis

  • Rheumatoid Arthritis

  • Ankylosing spondylitis

• Risk for liver injury

• Risk for renal impairment

Ketorolac

• NSAID

• Powerful analgesic – equivalent to opioids

• Mild anti-inflammatory effects

• Oral or parenteral

• Acute pain – moderate to severe

• Short term use only – 5 days

  • Increased risk of thrombotic events, renal failure, bleeding, peptic ulcers

• NSAID adverse effects

  • Peptic ulcer

  • GI bleeding renal impairment

Methotrexate

• First line treatment

• Most rapid-acting DMARD

• Therapeutic effect: 3 to 6 weeks

• Evaluate hepatic and renal function

• Adverse effects

  • Hepatic fibrosis

  • Bone marrow suppression

    • Risk for infection

  • GI ulceration

  • Pneumonitis

Etanercept

• Action

  • Inactivates TNF

• Tumor necrosis factor (TNF) inhibitors

  • Suppress immune function

  • Pose risk of serious infection

• Use

  • Moderate to severe rheumatoid arthiritis

Infliximab

• Immunomodulator

• Uses

  • Rheumatoid arthritis

  • Crohn’s disease

• Caution in hepatic dysfunction, active infection

Adalimumab

• Immunomodulator

• Uses

  • Rheumatoid arthritis

  • Psoriatic arthritis

  • Crohn’s disease

  • Ulcerative colitis

• Caution in active infection

Indomethacin

• NSAID

• Moderate to Severe gout

• Increases risk of MI or stroke even without risk factors

• GI irritation and bleeding risk

Colchicine

• Anti-inflammatory agent

  • No longer the first-line drug

  • Now reserved for patients who are unresponsive to or intolerant of safer agents

• Uses

  • Treats acute gouty attack

  • Reduces incidences of attack

  • Aborts an impending attack

  • NOT for long-term maintenance

Allopurinol

• Drug therapy for hyperuricemia

• Inhibits uric acid formation

• Inhibits xanthine oxidase (XO), an enzyme required for uric acid formation

Probenecid

• Drug therapy for hyperuricemia

• Increases uric acid excretion

Pegloticase

• Drug therapy for hyperuricemia

• Converts uric acid to allantoin, a compound readily excreted by the kidney

Probenecid

• Uricosuric

• Acts on renal tubules to inhibit reabsorption of uric acid

  • Prevents formation of new tophi and helps diminish existing tophi

  • May exacerbate acute episodes of gout

  • Add indomethacin for relief

• Take with food

Prednisone

• Glucocorticoid

• Anti-inflammatory

• Highly effective in relieving pain due to inflammation

• Useful for patients who are hypersensitive to, are unresponsive to, or have medical conditions that contraindicate the use of NSAIDs

• Avoid in patients prone to hyperglycemia

Calcitonin

• Osteoporosis treatment

• Thyroid hormone

• Opposes action of parathyroid hormone

Raloxifine

• Osteoporosis treatment

• Postmenopausal women

• Estrogen like effects w/o cancer risks

  • Osteoporosis

  • Breast cancer

• Risk for:

  • Deep vein thrombosis (DVT)

  • Pulmonary embolism

  • Stroke

• Pregnancy Category X

Tamoxifine

• Osteoporosis treatment

• Effects resemble those of estrogen

• Reduces bone resorption and turnover

Alendronate

• Most widely used biophosphonate

• Approved for

  • Post-menopausal osteoporosis

  • Male osteoporosis

  • Glucocorticoid induced osteoporosis

  • Paget’s disease

• Increases bone mineral density

  • Decreases number and activity of osteoclasts

• Orally administered but poor bioavailability

Alendronate adverse effects and contraindications

• Adverse effects

  • Generally well tolerated

  • Esophagitis is principal concern

    • Contraindicated in patients who cannot sit or stand for at least 30 min

    • PATIENT MUST SIT UP FOR 30 MIN AFTER ADMINISTRATION!!!

      • If the drug gets into the esophagus, it will destroy the esophagus

• Contraindication

  • Do NOT take with food as it decreases absorption

Pregabalin

• Lyrica

• Uses

  • Seizures

  • Neuropathic pain (DM, Fibromyalgia)

• Abuse potential

  • Euphoric effects

  • Schedule V

Baclofen

• Drug for spasticity

• No antidote for overdose

• CNS depressant

  • Drowsiness, dizziness, weakness, fatigue

  • Symptoms decrease with repeated use

    • Dose increased gradually

    • Do not use other CNS depressants (alcohol)

• NOT for spasticity r/t CVA

Abrupt discontinuation of baclofen administration via pump (intrathecal route)

• High fever

• Exaggerated rebound spasticity

• Rhabdomyolosis

• Multiple organ failure

• Death

Dantrolene

• Muscle relaxant

• Acts directly on skeletal muscle

• Makes muscle less able to contract by suppressing release of calcium

• Therapeutic uses

  • Spasticity r/t MS, Cerebral Palsy, Spinal cord injury (administered PO)

    • Causes significant reduction in muscle strength

• *Baclofen is preferred

Cyclobenzaprine

• Therapeutic use: relief of muscle spasm and associated pain

• Side effects:

  • Drowsiness, dizziness, fatigue

  • Dry mouth, blurred vision, photophobia

  • Urinary retention and constipation

  • Cardiac rhythm disturbances

  • Serotonin Syndrome – if combined with antidepressants

    • May be fatal

    • High fever, rhabdomyolysis, and seizures

Diazepam

• Member of the Benzodiazepine family

  • The only drug labeled to treat spasm and spasticity

• Mechanism of action

  • Acts in CNS

  • Mimics action of GABA

• Adverse effects

  • CNS depression (sedation)

  • Dependence

    • Withdrawn slowly