Exam 2 Prototype Drugs

vitamin A

• Retinol

• Fat-soluble

• Food sources

  • Beta-carotene

  • Plant based darkly color fruits/veggies

  • Carrots, cantaloupe, spinach

  • Retinoids

  • Animal origin dairy 

  • Meat

  • Fish

  • Fish oil 

• Function

  • Bone growth

  • Epithelial tissue

  • Skin

  • Eyes

  • Hair maintenance 

• Deficiency 

  • Night blindness, corneal dryness & ulceration

  • Skin lesions, dysfunction of mucous membranes 

• Excess doses 

  • Teratogenic effect

  • Liver damage 

  • Hypervitaminosis A: hair loss, peeling skin, GI upset, lethargy

vitamin C

• Water soluble

• Function

  • Essential antioxidant 

  • Forms collagen

• Food sources

  • Citrus fruits, cantaloupe, tomatoes, leafy green vegetables, green peppers, potatoes, strawberries, kiwi fruit

• Deficiency 

  • Poor wound healing

  • scurvy

• Excess doses 

  • GI upset

  • Crystalluria is taken with aspirin or sulfonamides 

  • Decreased effect oral anticoagulants

iron

• Food sources

  • Liver, lean meats, egg yolks, dried beans, spinach, fruit 

• Function 

  • Vital for hemoglobin regeneration

  • Treat iron deficiency anemia 

• Deficiency 

  • Anemia, fatigue, weakness, shortness of breath, pallor, GI bleeding 

• Toxicity 

  • Nausea, vomiting, diarrhea, GI bleeding, seizures

  • Liver toxicity= liver failure

  • Shock

  • BLACK BOX WARNING: serious cause of poisoning in children

  • Use bubble packs to keep out of reach

  • MEDICAL EMERGENCY: leads to fatal hemorrhagic shock and/or liver failure

chloroquine phosphate (antimalarial)

• Malaria treatment and prophylaxis (especially prior to foreign travel)

• Not recommended for treatment of SARS-COV-2/COVID19

• MOA

  • Inhibits parasite replication (DNA/RNA replication)

• Contraindications

  • Ocular disease

  • Hypersensitivity 

• Caution 

  • Cardiac, renal, liver, GI, neuro disease; alcoholism 

• Side effects

  • Retinal and visual field involvement

  • GI: N/V/D abdominal cramps, anorexia

  • Visual impairment, photosensitivity 

  • Hair & eye discoloration

  • Fatigue, headache, nervousness

• Adverse reactions

  • Cardiac: heart block/cardiac arrhythmias, EKG changes, hemolytic anemias 

  • Due to risk of seizures, dizziness avoid driving

  • Avoid sun exposure 

• Life threatening 

  • Absolute contraindication: allergy and ocular disease 

  • Loss of consciousness

  • Corneal opacity/ocular degeneration/macular degeneration (blindness)

  • Ototoxicity 

  • Cardiovascular collapse

  • Anaphylactic shock

ivermectin (antihelmintic/antiparasitic)

• Broad spectrum antiparasitic

• Action

  • Destroy parasitic worms

  • Usually given 1-3 days 

  • Few adverse reactions

  • Repeated doses may be necessary

• Caution 

  • Asthma

  • Liver impairment

  • Immunosuppressed persons

  • Not recommended with breast feeding

• Side effects

  • Dizziness

  • Drowsiness

  • Headache

  • Weakness

  • GI distress

• Adverse reactions

  • SJ syndrome

  • Seizures

  • Ocular hemorrhage/visual impairment/uveitis

  • Coma

metronidazole (peptide/amebicide)

• Synthetic antibiotic and antiprotozoal

• Effect/uses

  • Produces bactericidal, antiprotozoal, amebicidal, trichomonacidal effects

  • Trichomoniasis, bacterial vaginosis  

• Contraindications

  • First trimester pregnancy, breastfeeding, hematological disease

• Caution

  • Liver, cardiac, neoplastic disease 

• Side effects

  • Metallic taste, GI (N/V/D, abdominal cramps, anorexia, dry mouth), dizziness

  • With alcohol ingestion: disulfiram type reaction (disulfram is a drug used to treat alcoholism that causes unpleasant symptoms such as sweating, flushing, nausea, vomiting) 

• Adverse reactions 

  • Seizures, various immunosuppression concerns

  • TOXIC REACTIONS: neurological disturbances: seizures and peripheral neuropathies 

• Clinical judgement: immunity, infection

  • Monitor liver function, renal function, platelets, Hgb/Hct

  • Check urine function (monitor I & O)

  • Monitor for altered LOC (level of consciousness)

  • Check for super infections (candidiasis risk)

  • Clients should report decreased urination, urinary flow

aspirin

• Action

  • Inhibits prostaglandin synthesis

  • Anti inflammatory, antiplatelet, antipyretic effects

• Use

  • Most commonly as low dose to prevent blood clots (antiplatelet) 

  • Mild pain, fever

• Toxic serum salicylate level 

  • Greater than 300 mcg/mL

• Maximum dose 

  • 4 g/day 

• Caution

  • Do not take with other NSAIDs

  • Avoid last trimester of pregnancy

  • Do not give to children with flu or virus symptoms (reyes syndrome)

• Side effects

  • Dizziness

  • Lethargy

  • Headache 

  • Confusion and agitation

  • N and GI distress

  • Diaphoresis and dehydration

• Adverse reactions

  • Tinnitus

  • Hearing loss

  • hypo/hyperflycemia 

  • Reyes syndrome 

• Drugs

  • Increase bleeding with anticoagulants and other NSAIDs

  • Hypoglycemia w oral antidiabetics

  • Increases gastric ulcer risk w glucocorticoids

  • Decreases effects of ACE inhibitors, loop diuretics 

ibuprofen

• Most widely used NSAID

• Highly bound protein

• Action

  • Inhibits COX1 and COX2 by blocking arachidonate 

• Use

  • Pain, osteoarthritis, rheumatoid arthritis 

• Side effects

  • Dizziness

  • Drowsiness

  • Headache

  • Confusion

  • Blurred vision 

  • Edema

• Adverse reaction

  • Gastric distress  & bleeding

  • Hearing loss and tinnitus 

  • Anemia

  • SJ syndrome

• Drug interactions

  • Bleeding with warfarin

  • Increased effects w phenytoin, sulfonamides, warfarin 

  • Decreased effect w aspirin

celecoxib

• Action

• COX2 inhibitor 

• Use 

  • Pain, osteoarthritis, rheumatoid arthritis 

  • Painful dysmenorrhea 

  • Migraine 

• Food interactions

  • Ginkgo biloba may increase bleeding risk

• Caution

  • Pt’s w renal and hepatic dysfunction

• side/adverse effects

  • Headache, dizziness, sinusitis

  • N/V/D

  • GI bleeding, HTN (hypertension) 

  • Hearing loss

  • Anaphylaxis

infliximab

• Tumor necrosis factor blocker 

• Uses

  • Psoriasis 

  • Rheumatoid arthritis 

  • Ulcerative colitis 

  • Chron’s diseases

• GIVEN IV ONLY

• Caution

  • Pt’s w hepatic dysfunction, bone marrow suppression, DM, COPD

• Side/adverse effects:

  • Headaches, dizziness, cough, fatigue, chills, rash

  • Severe infections

  • Bronchospasm

  • Leukopenia

febuxostat

• Action

  • Blocks xanthine metabolism to reduce uric acid

  • Increases uric acid excretion

  • Prevents gout attacks 

• Uses

  • Gout 

  • Hyperuricemia 

• Caution

  • Pt’s w hepatic and renal disorder

  • Cardiac disease

  • Chemotherapy 

• side/adverse effects

  • Headache, dizziness, blurred vision

  • Bradycardia

  • Hyperglycemia 

  • N/V/D

  • Thrombocytopenia

acetaminophen

• Action

  • Inhibits prostaglandin synthesis

• Uses

  • Muscular aches & pain, fever

• drug/food interactions

  • Increased effect w caffeine 

  • Decreased effect w oral contraceptives, antacids 

• Side effects

  • Anxiety, headache

  • Insomnia, fatigue 

• Adverse reactions 

  • Oliguria

  • Hearing loss

  • hepatic/renal failure

  • Blood dyscrasias- anemia, thrombocytopenia

• Maximum dose: 4g/day

morphine sulfate

• Action

  • Depression of the CNS and pain impulses

• Uses

  • Moderate & severe pain

• drug/food interactions

  • Increased effect w alcohol 

  • Decreased effect with St. John’s wort 

• Side effects

  • Anorexia, dry mouth 

  • N/D, abdominal pain 

  • Constipation 

• Adverse reactions 

  • Orthostatic hypotension

  • bradycardia/tachycardia

  • Respiratory depression

  • Urinary retention

nalbuphine

• Action

  • Inhibits pain impulses to the CNS

  • Binds w opiate receptors and increases pain threshold

• Uses

  • Moderate and severe pain

  • Anesthesia induction

• drug/food interactions

  • Increased effect w alcohol and CNS depressants 

• Contraindication

  • Alcohol and drug disorders

  • Head injury

  • Increases IC

  • Older adults 

• Side effects 

  • Dizziness, drowsiness, headache

  • Dry mouth 

  • N/V

• Adverse reactions 

  • Bradycardia, dyspnea, hypo/hypertension

  • Respiratory depression, seizures

sumatriptan

• Antimigrane, selective serotonin receptor agonist

• Action

  • Inhibits pain impulses to the CNS

  • Binds w opiate receptors & increases pain threshold

• Uses

  • Treat migraine and cluster headaches

  • Vasoconstriction of cranial arteries

• Contraindication

  • CAD, PVD, HTN, DM

  • renal/hepatic dysfunction

  • Dysrhythmias in older adults

• Side effects

  • Dizziness, headache

  • Blurred vision, paresthesia 

• Adverse reactions 

  • hypo/hypertension

  • Coronary artery vasospasm

  • Dysrhythmias

  • Cardiac arrest

nystatin

• Treats cutaneous and mucocutaneous candida fungal infections

• Action: it binds to fungal cell membranes

• Oral administration, swish and swallow 

• Topical: usually a powder (small container, puff out onto skin 2x daily)

• Side effects:

  • Oral: N/V/D/ abdominal pain

  • Topical: contact dermatitis 

• Adverse reactions: hypersensitivity 

• Lifethreatening: Stevens-Johnson syndrome

fluconazole

• Indications

  • Treats all types of candidiasis, including systemic

  • Also treats cryptococcal meningitis 

• Route

  • Oral, IV, vaginal, topical

• Action

  • Increases cell permeability by inhibiting with ergosterol synthesis

• Side effects

  • Headache

  • Rash

  • GI distress (N/V/D/abd pain)

  • Hypokalemia 

• Adverse reactions 

  • Fatal cardiac dysrhythmias 

  • Hepatotoxicity 

  • Seizures

  • Leukopenia

diphenhydramine

Use

• allergic rhinitis

• pruritus

• urticaria

• common cold

• sneezing

• cough

• motion sickness prevention

interactions:

• increases CNS depression with alcohol & other CNS depressants

contraindications:

• closed angle glaucoma

• urinary retention

• sever liver disease

warnings:

• is used for histamine reactions

• common in OTC sleep aids

dextromethorphan hydrobromide

action:

• act on the cough control center in the medulla to suppress the cough reflex

types:

• nonopioid

• opioid

• combination preparations

fluticasone

action:

• anti-inflammatory

• decrease rhinorrhea, sneezing, and congestion

use:

• allergic rhinitis

side effects:

• headache

• blurred vision

• pharyngitis

• candidiasis

• insomnia

• irritated/dry nasal mucousa

• hoarseness

• N/V

albuterol

action:

• causes bronchodilation

• rapid onset of action

• INHALE: 5-15 min

• longer duration of action

• few side effects

use:

• asthma

• acute bronchospasm

• bronchospasm by prophylaxis

side effects:

• headache

• excitability

• tremors

• palpitations

• tachycardia

• rhinitis

tiotropium

use:

• maintenance treatment of bronchospasms associated with COPD

• not rescue

• administered by inhalation only with the HandiHaler device

side effects:

• dry mouth, constipation, GI distress

• depression, insomnia, headache

• pharyngitis, sinusitis, infection

• arthralgia, peripheral edema

montelukast

action:

• reduce inflammatory process & decrease bronchoconstriction

use:

• asthma

• prophylaxis of exercise induced bronchospasms

• not recommended for acute asthmatic attacks

common side effects:

• dizziness

• headache

• confusion

• GI distress

• depression

• weakness

• infection

amoxicillin

structure:

• beta-lactam ring

action:

• inhibit bacterial cell wall synthesis

• bacteriostatic & bactericidal

• depending upon drug and dosage

types:

• basic, broad spectrum, penicillinase-resistant, and extended spectrum

side/adverse effects:

• hypersensitivity, anaphylaxis

• superinfection

• tongue discoloration, stomatitis, glossitis

• GI distress

• arthralgia

• CDAD

drug interactions:

• increased effect with aspirin

• increased bleeding with oral anticoagulants

• decreased effects with acidic fruits and juices

ceftriaxone

structure:

• beta lactam structure

action:

• inhibit bacterial cell wall synthesis

• bactericidal

groups:

• first, second, third, fourth, and fifth generation

side/adverse effects:

• anaphylaxis

• superinfection

• headache, dizziness

• GI distress

• increased bleeding

• elevated hepatic enzymes

• nephrotoxicity

• CDAD

drug interactions:

• alcohol causes flushing, dizziness, headache, N/V, & muscular cramps

• anticoagulants may increase bleeding

• loop diuretics, aminoglycosides, and vancomycin may increase nephrotoxicity

azithromycin (macrolide)

use:

• broad spectrum macrolide antibiotic effective against numerous bacterial infections

action:

• Binds to 50S ribosomal subunits and inhibits protein synthesis; bacteriostatic at low-moderate doses, bactericidal at high doses

pharmacokinetics:

• Incompletely absorbed from GI tract (only 37% reaches systemic circulation); long half-life up to 68 hours allowing once-daily dosing; excreted in bile, feces, and urine

side effects:

• GI disturbances: Nausea, vomiting, diarrhea, abdominal cramping

• Conjunctivitis (avoid contact lenses if this occurs)

adverse reactions:

• CDAD

• hepatotoxicity

administration:

• orally or IV (MUST BE DILUTED)

isoniazid

use:

• first line treatment for tuberculosis

MOA:

• Bactericidal; inhibits tubercle cell wall synthesis and interferes with pyridoxine (vitamin B₆) metabolism

administration:

• oral

side effects:

• headaches

• GI distress, N/V

• Paresthesia

adverse reaction:

• hepatotoxicity

• blood dyscrasias

• ocular toxicity

• memory impairment

• hyperglycemia

• seizures

• hypotension

• neuropathy

clinical considerations:

• prescribe with INH to avoid vitamin B deficiency and minimize peripheral neuropathy

• combination therapy with other anti-tubercular drugs is needed