Exam 4 flashcards
Prednisone (Glucocorticoid - corticosteriod) (Short-Med Acting)
Effect:
- PMN increase
- Lymphocyte/monocyte/granulocyte decrease
- Decrease response to Ag
- Decrease release of mediators (IL1,2, TNF-a, collagenase/elastase)
- Inhibit Phospolipase A2 and COX2
- liver activation Use:
- allergic/hemato/collagen disorders
- hepatic/renal dz SE:
- short = nothing; see SE card
- long = iatrogenic Cushing’s, osteoporosis, infection, ulcers
Methylprednisone (Glucocorticoid - corticosteriod) (Short-Med Acting)
Effect:
- PMN increase
- Lymphocyte/monocyte/granulocyte decrease
- Decrease response to Ag
- Decrease release of mediators (IL1,2, TNF-a, collagenase/elastase)
- Inhibit Phospolipase A2 and COX2 Use:
- allergic/hemato/collagen disorders
- hepatic/renal dz SE:
- short = nothing
- long = iatrogenic Cushing’s, osteoporosis, infection, ulcers
Cyclophosphamide (Prodrug - cytotoxic/antiprolif. T/B cell)
Effect:
- Alkylating agent, signal 3 inhib.
- Non-cell cycle spec
- Inhib B/T Cell (direct cytotox=immune supp.) Use:
- RA
- Leukemia SE:
- Short term = N/V
- Long term = Bone Marrow Supp. (leukopenia, thrombocytopenia, anemia)
- Derm (alopecia)
Azathioprine (cytotoxic/antiprolif. T/B cell)
Effect:
- Antimetabolite, Signal 3 inhib.
- Cell-cycle spec
- Inhib T > B Use:
- Renal Allotrasplant.
- RA (ADULT ONLY) SE:
- Short term = N/V/D
- Long term = Bone Marrow supp. (leukopenia, thrombocytopenia, macrocytic anemia)
- Infections
Methotrexate (cytotoxic/antiprolif. T/B cell)
Effect:
- Antimetabolite, Signal 3 inhib.
- Cell-cycle spec
- Inhibit B/T cell Use:
- Crohn’s
- RA
- Leukemia SE:
- N/V
- Bone Marrow Supp.
- Hepatox.
Mycophenolate Mofetil (T-cell supp)
Effect:
- Inhib Purine synth, Signal 3 inhib.
- Inhibit B/T cell Use:
- Kidney/Liver/Heart rejection
- combo w/ cyclosporine/cortico SE:
- GI
- neutropenia
- infection
Cyclosporine (T-cell supp)
Effect:
- Inhibit calcineurin and Signal 1
- T-cell supp. Use:
- Kidney/Liver/Heart rejection
- w/ cortico/azathiprine
- RA SE:
- Nephrotox
- HTN
- Embryotox
Muromonab-CD3 (Murine - T-cell supp)
Effect:
- Inhibit CD3R and Signal 1
- T-cell supp. Use:
- Kidney/Liver/Pancreas/Heart rejection SE:
- Fever/Chills
- Murine sensitivity
Lymphocyte Immune Globulin (Horse - T-cell supp)
Effects:
- T-cell supp. Use:
- Kidney rejection SE:
- fever/chills
- horse sensitivity
Daclizumab (Human - T-cell supp)
Effect:
- Inhibit IL-2R and Signal 3 Use:
- Kidney rejection SE:
- GI dysfunction
RHO Immune Globulin (Human - Ab immunosupp.)
Effect:
- Supp immune response to Rh+ RBCs Use:
- prevent erythroblastosis fetalis SE:
- mild
- contra for Rh+ pts
Immune Globulin (Human - Replacement tx)
Effects:
- increase passive immunity Use:
- Hypogammaglobulinemia
- Prevent infections in HIV+ SE:
- mild
Interferon Beta-1b (Immunomodulators)
Effects:
- Antiviral/Immunoregulatory Use:
- MS (relapsing-remitting) SE:
- Flu-like S/S
- depression/suicide
- injection site rxn
Interferon Gamma (Immunomodulators)
Effects:
- activate phagocytic activity
- Ab-dependent cytotox. Use:
- chronic granulomatous dz
- osteoporosis SE:
- Flu-like S/S
Acetyl Salicylic Acid (Salicylic Acid Deriv.)
- pKa = 3.5 (acidic)
- Abs favored in LI b/c large SA (even though not favored by kinetics)
- Kidney excretion; if you increase urine pH = increase excretion Effects:
- Irreversible COX 1/2 inhibition Use:
- Analgesic
- Anitpyretic
- Antiinflamm
- Antirheumatic
- prevent A/V thrombosis SE:
- GI - inhibit COX1 .: no PGs (protection) leads to S/S
- Tinnitus
- Heptic
- Renal ischemia due to PG inhibition
- Decrease Hct/Fe serum conc. + decrease RBC lifespan
- Hypersensativity - urticaria/angioedema
- Reye’s (children) Rx Interactions
- protein bound
- anticoagulants
- corticosteroids
- NSAIDs
Diflunisal (Salicylic Acid Deriv.)
Effects:
- Reversible COX1/2 inhibit Use: Analgesic (acute/chronic mild-mod) Antiinflamm RA/Osteoarthritis SE:
- Mild GI
- HA
- Renal
- Hypersensativity
Indomethacin (Acetic Acid Deriv.)
Effects:
- Reversible COX 1/2 inhibition Use:
- RA
- Osteoarthritis
- Tocolytic agent SE:
- Severe GI
- Prolong Gestation
- Renal
- HA + aggrevated depression
Etodolac (Acetic Acid Deriv.)
Effects: COX 2 > COX 1 inhibition Use: RA Osteoarthritis Post op analgesia (6-8h) SE: GI (Less severe)
Diclofenac (Acetic Acid Deriv.)
Effect:
- Reversible COX1/2 inhibition Use:
- RA
- Osteoarthritis
- Analgesia/Dysmenorrhea SE:
- GI
- Dizziness + HA
Tolmetin (Acetic Acid Deriv.)
Effect:
- Reversible COX1/2 inhibition Use:
- JRA
- RA
- Osteoarthritis SE:
- GI
- HA
- anaphylaxis
Ketorolac (Acetic Acid Deriv.)
Effect:
- Reversible COX1/2 inhibition Use:
- Mod-sev acute pain SE:
- GI
- HA
Ibuprofen (Proprionic Acid Deriv.)
Effect:
- Reversible COX1/2 inhibition Use:
- RA
- Osteoarthritis
- Analgesia
- Dysmenorrhea
- Fever SE:
- Mild GI
- Ocular dysfunction
- Rash/Dermatitis
- Contra: preggo/milking
Naproxen (Proprionic Acid Deriv.)
Effects:
- Reversible COX1/2 inhibition Use:
- JRA
- RA
- Osteoarthiritis
- Anagesia
- Dysmenorrhea SE:
- Mild GI
- HA
- Hypersensitivity
Ketoprofen (Proprionic Acid Deriv.)
Effects:
- Reversible COX1/2 inhibition Use:
- RA
- Osteoarthritis
- Analgesia
- Dysmenorrhea SE:
- GI - 30% of pts
- HA
Oxaprozin (Proprionic Acid Deriv.)
Effects:
- Reversible COX1/2 inhibition - Used Once daily Use:
- RA
- Osteoarthritis SE:
- GI
Piroxicam (Enolic Acid Deriv. - Oxicams)
Effects:
- Reversible COX1/2 inhibition Use:
- RA
- Osteoarthritis SE:
- GI
Meloxicam (Enolic Acid Deriv. - Oxicams)
Effects:
- Reversible COX 2 > 1 inhibition Use:
- Osteoarthritis SE:
- GI
Nabumetone (Non-acidic)
Effect:
- Reversible COX 2 > 1 inhibition Use:
- RA
- Osteoarthritis SE:
- GI
- HA
Celecoxib (COX-2 Inhibitor)
Effect:
- Selective COX 2 inhibition Use:
- Osteoarthritis
- RA
- dysmenorrhea
- acute pain
- familial adenomatous polyposis SE (all minor):
- GI (less than COX 1 inhibitors)
- HA and dizziness
- Respiratory
- Rash
- Sulfonamide allergy
Acetaminophen
Effect:
- analgesia (increase pain threshold)
- weak COX1/2 inhibition
- antipyresis via reg. @ hypothalamic heat-reg center Use:
- analgesia
- antipyretic
- Osteoarthritis SE:
- Heptotox
- Nephrotox
- Rash (minor)
Epinephrine (Adrenergic Bronchodilator)
Effect:
- Bronchodilation
- inhibit degranulation from mast cells Use:
- acute asthma attacks/asthmatic bronchospasms
- anaphylactic reactions SE:
- CNS stimulation
- Cardiac stimulation
- tolerance/rebound bronchospasm
Isoproterenol (Adrenergic Bronchodilator)
Effect:
- Bronchodilation
- inhibit degranulation from mast cells Use:
- acute asthma attacks/asthmatic bronchospasms
- anaphylactic reactions SE:
- CNS stimulation
- Cardiac stimulation
- tolerance/rebound bronchospasm
Metaproterenol (Adrenergic Bronchodilator)
Effect:
- Bronchodilation
- inhibit degranulation from mast cells Use:
- acute asthma attacks/asthmatic bronchospasms
- anaphylactic reactions SE:
- CNS stimulation
- Cardiac stimulation
- tolerance/rebound bronchospasm
Albuterol/Levalbuterol (Adrenergic Bronchodilator)
Effect:
- Bronchodilation
- inhibit degranulation from mast cells Use:
- acute asthma attacks/asthmatic bronchospasms
- anaphylactic reactions SE:
- CNS stimulation
- Cardiac stimulation
- tolerance/rebound bronchospasm
Salmeterol (Adrenergic Bronchodilator)
Effect:
- Bronchodilation
- inhibit degranulation from mast cells Use:
- acute asthma attacks/asthmatic bronchospasms
- anaphylactic reactions SE:
- CNS stimulation
- Cardiac stimulation
- tolerance/rebound bronchospasm
Terbutaline (Adrenergic Bronchodilator)
Effect:
- Bronchodilation
- inhibit degranulation from mast cells Use:
- acute asthma attacks/asthmatic bronchospasms
- anaphylactic reactions SE:
- CNS stimulation
- Cardiac stimulation
- tolerance/rebound bronchospasm
Pirbuterol (Adrenergic Bronchodilator)
Effect:
- Bronchodilation
- inhibit degranulation from mast cells Use:
- acute asthma attacks/asthmatic bronchospasms
- anaphylactic reactions SE:
- CNS stimulation
- Cardiac stimulation
- tolerance/rebound bronchospasm
Theophylline (Methylxanthine Bronchodilator)
Narrow therapeutic window Not used b/c of SEs Effect: bronchodilation inhibit mast cell degranulation inhibit PDE4 -> increase cAMP in mast cell and smooth muscle interact with adenosine receptors Use: oral in conjunction with other Rx for severe asthma SE: Mild: N/V, HA, insomnia, nervousness Severe: arrhythmias, seizures
Aminophylline (Methylxanthine Bronchodilator)
- Narrow therapeutic window
- Not used b/c of SEs Effect:
- bronchodilation
- inhibit mast cell degranulation
- inhibit PDE4 -> increase cAMP in mast cell and smooth muscle
- interact with adenosine receptors Use:
- IV for severe asthma SE:
- Mild: N/V, HA, insomnia, nervousness
- Severe: arrhythmias, seizures
Beclomethasone (Corticosteroid)
Effects:
- antiinflammatory
- inhibit leukocyte recruitment
- inhibit synthesis/release of PGs, TXs, leukotrienes, PAFs, etc.
- reduce cell mediated bronchial epithelial damage
- slow acting Use:
- prophylactic NOT acute SE:
- Cataracts (inhaled steroids)
- Cushing Syndome
- Immunosuppression
- Osteoporosis
- Peptic ulcer
- Growth suppression in kids (systemic use)
- Hypothalamic-Pit axis suppression
- Menstrual/repro problems
Flunisolide (Corticosteroid)
Effects:
- antiinflammatory
- inhibit leukocyte recruitment
- inhibit synthesis/release of PGs, TXs, leukotrienes, PAFs, etc.
- reduce cell mediated bronchial epithelial damage
- slow acting Use:
- prophylactic NOT acute SE:
- Cataracts (inhaled steroids)
- Cushing Syndome
- Immunosuppression
- Osteoporosis
- Peptic ulcer
- Growth suppression in kids (systemic use)
- Hypothalamic-Pit axis suppression
- Menstrual/repro problems
Triamcinolone (Intermediate-acting Glucorticoid)
Effects:
- antiinflammatory
- inhibit leukocyte recruitment
- inhibit synthesis/release of PGs, TXs, leukotrienes, PAFs, etc.
- reduce cell mediated bronchial epithelial damage
- slow acting
- no mineralcorticoid activity Use:
- prophylactic NOT acute
- intralesional
- allergic rhinitis
- ophthalmic
- bronchial asthma
- oral ulcerative lesions
- adrenocortical insuff,
- DZ: derm, endocrine, GI, hem/neo, NS, nephro, rheumatic , resp, SLE SE:
- Cataracts (inhaled steroids)
- Cushing Syndome
- Immunosuppression
- Osteoporosis
- Peptic ulcer
- Growth suppression in kids (systemic use)
- Hypothalamic-Pit axis suppression
- Menstrual/repro problems
Fluticasone
Effects:
- antiinflammatory
- inhibit leukocyte recruitment
- inhibit synthesis/release of PGs, TXs, leukotrienes, PAFs, etc.
- reduce cell mediated bronchial epithelial damage
- slow acting Use:
- prophylactic NOT acute SE:
- Cataracts (inhaled steroids)
- Cushing Syndome
- Immunosuppression
- Osteoporosis
- Peptic ulcer
- Growth suppression in kids (systemic use)
- Hypothalamic-Pit axis suppression
- Menstrual/repro problems
Budesonide (Corticosteroid)
Effects:
- antiinflammatory
- inhibit leukocyte recruitment
- inhibit synthesis/release of PGs, TXs, leukotrienes, PAFs, etc.
- reduce cell mediated bronchial epithelial damage
- slow acting Use:
- prophylactic NOT acute SE:
- Cataracts (inhaled steroids)
- Cushing Syndome
- Immunosuppression
- Osteoporosis
- Peptic ulcer
- Growth suppression in kids (systemic use)
- Hypothalamic-Pit axis suppression
- Menstrual/repro problems
Mometasone (Corticosteroid)
Effects:
- antiinflammatory
- inhibit leukocyte recruitment
- inhibit synthesis/release of PGs, TXs, leukotrienes, PAFs, etc.
- reduce cell mediated bronchial epithelial damage
- slow acting Use:
- prophylactic NOT acute SE:
- Cataracts (inhaled steroids)
- Cushing Syndome
- Immunosuppression
- Osteoporosis
- Peptic ulcer
- Growth suppression in kids (systemic use)
- Hypothalamic-Pit axis suppression
- Menstrual/repro problems
Ciclesonide (Corticosteroid)
Effects:
- antiinflammatory
- inhibit leukocyte recruitment
- inhibit synthesis/release of PGs, TXs, leukotrienes, PAFs, etc.
- reduce cell mediated bronchial epithelial damage
- slow acting Use:
- prophylactic NOT acute SE:
- Cataracts (inhaled steroids)
- Cushing Syndome
- Immunosuppression
- Osteoporosis
- Peptic ulcer
- Growth suppression in kids (systemic use)
- Hypothalamic-Pit axis suppression
- Menstrual/repro problems
Cromolyn Sodium (Mast Cell Stabilizer)
Effect:
- inhibit degranulation Use:
- prophylaxis of bronchial asthma in conjunction with other agents
- rhinitis, conjunctivitis, GI allergies SE: (rare)
- throat irritation
- cough
- dry mouth
- wheezing
- HA
- bronchospams
- laryngeal edema
- rash
Monteleukast (Leukotriene Modulator)
Effects:
- Cysteinyl leukotriene receptor antagonist Use:
- oral
- decrease frequency/severity of asthma attacks
- Seasonal allergies
Zafirleukast (Leukotriene Modulator)
Effects:
- Cysteinyl leukotriene receptor antagonist Use:
- oral
- decrease frequency/severity of asthma attacks
- Seasonal allergies
Zileuton (Leukotriene Modulator)
Effects:
- 5-lipoxygenase inhibitor Use:
- oral
- decrease frequency/severity of asthma attacks
- 4x daily SE:
- Heptatotox
- liver enzyme elevation
Ipratropium (Antimuscarinic)
Effect:
- prevent Ach induced bronchospasm
- Quarternary salt; poor abs .: few systemic effects SE:
- dry secretions
Tiotropium (Antimuscarinic)
Effect:
- prevent Ach induced bronchospasm
- COPD SE:
- dry secretions
Aclidinium (Antimuscarinic)
Effect:
- prevent Ach induced bronchospasm
- COPD SE:
- dry secretions
Advair Diskus (Combo prep)
Salmeterol + Fluticasone
Combivent (Combo prep)
Ipratropium + Albuterol
Symbicort (Combo prep)
Formoterol + Budesonide
Dulera (Combo prep)
Formoterol + Mometasone
Omalizumab (Anti-IgE)
Diphenhydramine (H1 Antagonist - Sedating)
Effect:
- block H1 receptors Use:
- allergies
- rhinitis
- dermatitis
- NOT bronchospastic conditions
- antiemetic - vestibular system/CRTZ
- antitussive
- Sedation SE:
- dry secretions
Fexofenadine (H1 Antagonist - Non-sedating)
Effect:
- block H1 receptors Use:
- rhinitis
- dermatitis
- NOT bronchospastic conditions SE:
- dry secretions
Cetirizine (H1 Antagonist - Non-sedating)
Effect:
- block H1 receptors Use:
- rhinitis
- dermatitis
- NOT bronchospastic conditions SE:
- dry secretions
Loratidine (H1 Antagonist - Non-sedating)
Effect:
- block H1 receptors Use:
- rhinitis
- dermatitis
- NOT bronchospastic conditions SE:
- dry secretions
GLUCOCORTICOIDS (Effects)
2 types of negative feedback on ACTH secretion enhance Glc production stim hepatic gluconeogenesis decrease periph Glc utilization increase proteolysis/AA release (periph/intestial tissues) enhance FA mobilization/lipolysis/FA + glycerol release/choleserol synth potentiate adrenergic VC on small vessels decrease histamine release -> decrease capillary perm. increase plasma [Hb] increase plasma RBCs, WBCs, PMNs decrease eosinophils, basophils, monocytes, lymphocytes induce lipocortin production -> inhibits phospholipase A2 => decrease PGs/Leukotrienes decrease inflamm mediator release
GLUCOCORTICOID - SE
- decrease gastric mucus barrier -> bleeding/ulcers
- Edema
- Hyperglycemia
- increased serum TAGs
- hypokalema -> arrhythmias
- metabolic alkalosis
- hypophosphatemia ->mm weakness/cardiac dys/hemolysis
- osteonecrosis (femoral head)
- negative nitrogen balance
- insomnia, inc appetite, nervousness, irritability, sleep change, psychotic episodes
- growth supp.
- myopathy (protein catabolism)
- skin thinning + purpura
- SCC/BCC
- acne, alopecia, hypertrichosis, striae
- Cushingoid features
- inc IOP (decreased outflow)
- enhanced ocular infections/perforations
- cataracts
- increase infection risk - reactivate TB
- HPA supp.
- Fetus - cross placenta = cleft palate, fetal renal hypoplasia
Hydrocortisone (Short-Med Acting)
- GLUCOCORTICOID Effect:
- See Glucocorticoid effect card
- strong mineralcorticoid activity
- 1-2hr half-life
- urine excretion Use:
- adrencortical insuff
- anti-inflamm
- relief of inflamm to corticosteroid responsive dermatoses
- ulcerative colitis SE:
- See SE card
Dexamethasone (Long-acting Glucocorticoid)
Effect:
- hepatic meta
- no mineralcorticoid activity
- 5+ hr half-life
- urine/feces excretion Use:
- anti-inflamm
- immunosupp.
- Allergies
- bacterial meningitis (before ABX)
- collagen disorders (acute exacerbations) - SLE
- idiopathic hemolytic anemia/ITP
- Respiratory distress syndrome
- conjunctivitis
- otic inflammation SE:
- see SE card
Metyrapone (Glucocorticoid synth inhibitor + antagonist)
Effect:
- inhibits cortisol and aldosterone Use:
- hypersecretion of adrenalcorticoids
Ketoconazole (Glucocorticoid synth inhibitor + antagonist + Antifungal)
Effects:
- block all sterioid biosynthesis Use:
- Cushing’s disease
- antifungal
- acts synergistically w/ metyrapone
Fludrocortisone (mineralocorticoid agonist)
Effect:
- control renal excretion of cations
- promote reabsorption of Na in distal tubules - maintain blood volume
- increase Na/K ATPase
- enchance K/H+ excretion
- hepatic meta
- urine/feces excretion
- 30min half-life Use:
- aldosterone replacement
- Adrenocortical insuff. - Addison’s SE:
- hypokalemia
- metabolic alkalosis
- increase plasma volume
- HTN/edema
- convusions, HA, dizziness
- acne, rash, bruising
- growth supp.
- HPA supp
- hyperglycemia
- peptic ulcer
- mm weakness
- cataracts
Spironolactone (mineralocorticoid antagonist)
Effect:
- competes w/ aldosterone
- increase Na/H2O excretion
- conserve K/H+
- block aldosterone @ arteriolar sm
- hepatic meta
- 10 min half-life Use:
- manage edema from excessive aldosterone excretion
- HTN
- CHF
- 1˚ hyperaldosteronism
- hypokalemia
- cirrhotic liver SE:
- Edema
- drowsy, lethargy, HA, confusion, fever, ataxia, fatigue
- rash, urticaria, hirsutism, eosinophilia
- gynecomasta
- hyperkalemia, hyponatremia, dehydration
- amenorrhea, postmenopausal bleed
- agranulocytosis
- hepatotox
- increased BUN
Doxylamine (H1 Antagonist - Very Sedating)
Effect:
- H1 competative antagonist
- reduce severity of histamine stim: pain, itch, flare, VD, vasc perm increase, and congestion
- NO inhibition of mediator release
- NO reversal of anaphylactic bronchospasm Use:
- Allergies - Rhinitis, sneezing, wheezing, itchy eye/nose/throat, dermatitis
- Cold - nasal irritation
- Sedation
- decrease resp sec
- anticholinergic - parkinson’s SE:
- anticholinergic
- sedation,drowsy,confusion,amnesia,behavior change
- paradoxic CNS stim (kids)
- rash
- interfere w/ allergy testing
Promethazine hydrochloride (H1 Antagonist - Very Sedating)
Effect:
- H1 competative antagonist
- reduce severity of histamine stim: pain, itch, flare, VD, vasc perm increase, and congestion
- NO inhibition of mediator release
- NO reversal of anaphylactic bronchospasm Use:
- Antitussive
- Allergies - Rhinitis, sneezing, wheezing, itchy eye/nose/throat, dermatitis
- Cold - nasal irritation
- Antiemetic - motion sick/vert + N/V in preggo - vestibular system/CRTZ
- Sedation
- decrease resp sec
- anticholinergic - parkinson’s SE:
- anticholinergic
- sedation, drowsy, confusion, amnesia, behavior change
- paradoxic CNS stim (kids)
- rash
- interfere w/ allergy testing
Hydroxine (H1 Antagonist - Very Sedating)
Effect:
- H1 competative antagonist
- reduce severity of histamine stim: pain, itch, flare, VD, vasc perm increase, and congestion
- NO inhibition of mediator release
- NO reversal of anaphylactic bronchospasm Use:
- Allergies - Rhinitis, sneezing, wheezing, itchy eye/nose/throat, dermatitis
- Cold - nasal irritation
- Antiemetic - motion sick/vert + N/V in preggo
- Sedation
- decrease resp sec
- anticholinergic - parkinson’s SE:
- anticholinergic
- sedation, drowsy, confusion, amnesia, behavior change
- paradoxic CNS stim (kids)
- rash
- interfere w/ allergy testing
Dimenhydrinate (H1 Antagonist - Sedating)
Effect:
- H1 competative antagonist
- reduce severity of histamine stim: pain, itch, flare, VD, vasc perm increase, and congestion
- NO inhibition of mediator release
- NO reversal of anaphylactic bronchospasm Use:
- Allergies - Rhinitis, sneezing, wheezing, itchy eye/nose/throat, dermatitis
- Cold - nasal irritation
- Antiemetic- vestibular system/CRTZ
- decrease resp sec
- anticholinergic - parkinson’s SE:
- anticholinergic
- sedation, drowsy, confusion, amnesia, behavior change
- paradoxic CNS stim (kids)
- rash
- interfere w/ allergy testing
Chlorpheniamine maleate (H1 Antagonist - Sedating)
Effect:
- H1 competative antagonist
- reduce severity of histamine stim: pain, itch, flare, VD, vasc perm increase, and congestion
- NO inhibition of mediator release
- NO reversal of anaphylactic bronchospasm Use:
- Allergies - Rhinitis, sneezing, wheezing, itchy eye/nose/throat, dermatitis
- Cold - nasal irritation
- decrease resp sec
- anticholinergic - parkinson’s SE:
- anticholinergic
- sedation, drowsy, confusion, amnesia, behavior change
- paradoxic CNS stim (kids)
- rash
- interfere w/ allergy testing
Meclizine (H1 Antagonist - Sedating)
Effect:
- H1 competative antagonist
- reduce severity of histamine stim: pain, itch, flare, VD, vasc perm increase, and congestion
- NO inhibition of mediator release
- NO reversal of anaphylactic bronchospasm Use:
- Allergies - Rhinitis, sneezing, wheezing, itchy eye/nose/throat, dermatitis
- Cold - nasal irritation
- Antiemetic - motion sick/vert- vestibular system/CRTZ
- decrease resp sec
- anticholinergic - parkinson’s SE:
- anticholinergic
- sedation, drowsy, confusion, amnesia, behavior change
- paradoxic CNS stim (kids)
- rash
- interfere w/ allergy testing
Cimetidine (H2 - Antagonist)
Effect:
- competative H2 antagonist - inhibit gastric acid sec. (response to vagal stim, gastrin, stress) Use:
- duo/gastric/stress ulcer
- GERD
- ZES
- pre-op; dec aspiration damage SE:
- HA, dizzy, nausea, rash, itching (elderly w/ renal dz)
- antiandrogenic - dec. libido, impotence, gynecomastia
- cytopenias
- increase [creatinine]
- Drug interactions: inhibit hepatic microsomal drug enzymes and alter gastric pH
Ranitidine (H2 - Antagonist)
Effect:
- competative H2 antagonist - inhibit gastric acid sec. (response to vagal stim, gastrin, stress) Use:
- duo/gastric/stress ulcer
- GERD
- ZES
- pre-op; dec aspiration damage SE:
- HA, dizzy, nausea, rash, itching (elderly w/ renal dz)
- Drug interactions: inhibit hepatic microsomal drug enzymes and alter gastric pH
Famotidine (H2 - Antagonist)
Effect:
- competative H2 antagonist - inhibit gastric acid sec. (response to vagal stim, gastrin, stress) Use:
- duo/gastric/stress ulcer
- GERD
- ZES
- pre-op; dec aspiration damage SE:
- HA, dizzy, nausea, rash, itching (elderly w/ renal dz)
- Drug interactions: inhibit hepatic microsomal drug enzymes and alter gastric pH
Nizatidine (H2 - Antagonist)
Effect:
- competative H2 antagonist - inhibit gastric acid sec. (response to vagal stim, gastrin, stress) Use:
- duo/gastric/stress ulcer
- GERD
- ZES
- pre-op; dec aspiration damage SE:
- HA, dizzy, nausea, rash, itching (elderly w/ renal dz)
- Drug interactions: inhibit hepatic microsomal drug enzymes and alter gastric pH
Scopolamine
- Transderm prep - prevents some SEs Effects:
- antimuscarinic
- act on vestibular system Use:
- vertigo and motion sickness SE:
- anticholinergic
- sedation, confusion, amnesia
Prochlorperazine (phenothiazine)
antiemetic
Metoclopramide
Effect:
- DA antagonist @ CRTZ
- increase GI tone and motility
- increase tone of lower eso sphincter Use:
- antiemetic - chemo/radiation
- GERD
- preop - aspiration vomitus SE:
- sedation
- extrapyramidal motor dys
Ondansetron (5-HT3 antagonist)
Effect:
- depress CRTZ
- inhibit seratonin med aff input to GI Use:
- antiemetic - chemo and postop N/V SE:
- drug interaction - hepatic enzyme meta
- HA
- Constipation
Granisetron (5-HT3 antagonist)
Effect:
- depress CRTZ
- inhibit seratonin med aff input to GI Use:
- antiemetic - chemo and postop N/V SE:
- drug interaction - hepatic enzyme meta
- HA
- Constipation
Dronabinol (THC)
Use:
- antiemetic - chemo SE:
- sedation
- confusion
- disorientation
- Loss of control
- altered sensation
- paranoia
- pyschosis
- Munchies! - good and bad
Aprepitant
- expensive Effect:
- P/neurokinin receptor (NK1) antagonist
- inhibit gastric motility and fxn Use: antiemetic - chemo SE:
- well tolerated
Opioid - Codeine/Hydrocodone
Use:
- most effective antitussive
- lower dose than analgesic SE:
- sedation
- light headedness
- confusion
- nausea
- dizzy
- constipation
- Abuse potential - dependence
Dextromethorphan
- Non-opiod Effect:
- block NMDA receptors in cough center Use:
- antitussive - mild/mod
- lower abuse potential than codeine SE:
- Mild: sedation, dizzy, confusion
Benzonatate
Effect:
- local anesthetic - desens. receptors in airway
- some effect @ cough center Use:
- antitussive SE:
- Mild: constipation, nasal congestion, nausea, drowsy, rash
Guaifenesin (Expectorant)
Effect:
- irritate GI -> activate reflexes -> increase mucus in airway Use:
- antitussive
Acetylcysteine (Mucolytic)
Effect:
- break mucus plug
- disrupt disulfide link -> decrease viscosity Use:
- antitussive
- following: surgery, tracheotomy, severe bronch., emphysema
- Acetaminophen antidote
Hydroxychloroquine sulfate (Non-biologic DMARD)
Effect:
- rapid GI abs
- Half-life: 6-7d
- deposit in tissues (eyes, brain, liver, spleen, lung, kidney, heart) Use:
- 2nd-line for moderate RA w/ methotrexate
- SLE
- Antimalarial SE:
- Ocular Tox
- pigmentation/psoriasis
- Contra: Preggo
- hypersensativity
Sulfasalzine (Non-biologic DMARD)
Effect:
- Immunosupp.
- CT affinity
- High conc. in liver/intestines Use:
- RA w/ hydroxychloroquine + parentral gold + methotrexate
- Chronic ulcerative colitis SE:
- reversible neutropenia
- Anorexia
- HA
- vomiting
- gastric distress
Leflunomide (Non-biologic DMARD)
Effect:
- inhibit pyrimidine synth
- inhibit dihydroorotate dehydrogenase Use:
- RA (adult) SE:
- Diarrhea
- elevated ALT/AST
- immunosuppression
- rash/alopecia
Etanercept (Biologic DMARD)
Effect:
- Bind TNF a/b; inhibit receptor binding
- mod TNF dependent activities Use:
- RA
- JRA
- combo w/ methotrexate SE:
- hypersensativity
- discontinue in pt w/ sepsis/infections
Infliximab (Biologic DMARD)
Effect:
- Neutralize TNF-a NOT b
- inhibit TNF-a dep activities Use:
- RA
- Crohn’s
- combo w/ methotrexate SE:
- hypersensativity
- immunosupp.
- infection
- HACA Abs
Levothyroxine (Hypothyroidism)
Effect:
- T4 converted to T3 in periph.
- increase dose for preggos or pts on estrogen tx Use:
- hypothyroidism
131I (Hyperthyroidism)
Effect:
- thyroid uptakes radioisotope -> damages tissue Use:
- Hyperthyroidism
- thyroid cancer SE:
- low cancer risk
- contra: nursing mommies
Propylthiouracil (Hyperthyroidism)
Effect:
- inhibit iodination reactions (3rd step)
- Inhibit iodotyrosines (4th step)
- does not inhibit release of preformed T3/T4
- block T4->T3 conversion: periph effects before T3/T4 depletion Use:
- hyperthyroidism
- good for preggos - more protein binding SE:
- Rash
- arthralgia
- heptatotox - minor/reversible
- Agranulocytosis - fatal
- vasculitis - rare
- lupus rxn - rare
Methimazole (Hyperthyroidism)
Effect:
- inhibit iodination reactions (3rd step)
- Inhibit iodotyrosines (4th step)
- does not inhibit release of preformed T3/T4 Use:
- hyperthyroidism
- periph effects before T3/T4 depletion SE:
- Rash
- arthralgia
- heptatotox - minor/reversible
- Agranulocytosis - less than PTU
- vasculitis - rare
- lupus rxn - rare
KI (Lugol’s Solution) (Hyperthyroidism)
Effects:
- 5% iodine + 10% K
- competative uptake of Iodine
- inhibit hormone synth (block 1st step)
- inhibit release of preformed hormone (6th step) Use:
- radioactive disaster
- conjunction w/thionamides
- temporary effects
- thyroid storm tx SE:
- Rash
- salivary gland swelling
- metallic taste
- sore teeth
Alendronate (Osteoporosis, Paget’s)
Effects:
- inhibit bone resorption w/o impairing mineralization Use:
- Paget’s - last for mos, good pain reduction
- osteoporosis - increased bone density/decrease fractures SE:
- GI distress
- esophageal erosion
- take w/ large glass of H2O + sit upright for 30 min
Risedronate (Osteoporosis)
Effects:
- binds hydroxyapetite in bone - decrease turnover Use:
- Paget’s - increase bone density
- osteoporosis SE:
- GI distress
- esophageal erosion
- Take w/ large glass H2O + sit upright for 30 min
Ibandronate (Osteoporosis)
Effects: decrease bone turnover Use: 1x/mo dose osteoporosis SE: GI distress Esophageal erosion high dose - constipation, flu-like S/S, extremity pain
Zoledronic Acid (Osteoporosis, Hypercalcemia, Paget’s)
Effects:
- very potent osteoclast inhibitor Use:
- IV - 1x/y SE:
- fever
- N/V/D
- constipation
- GI pain
- osteonecrosis of jaw
Teriparatide (Osteoporosis)
Effects:
- PTH - increase osteoblast activity -> increase Ca deposition
- increase bone formation in spine and femoral neck Use:
- osteoporosis
- SubQ injection, 1x/d, expensive SE:
- osteosarcoma
- nausea
- dizziness
- leg cramps
Raloxifene (Osteoporosis)
Effect:
- selective estrogen receptor modulation - bone agonist and breast/uterus antagonist (no cancer risk) Use:
- osteoporosis
- postmenopasual women SE:
- venous thromboembolism
Calcitriol (Osteoporosis, Hypoparathyroidism)
Effects:
- potent VitD metabolite - increase Ca abs and decrease Ca/phos excretion
- decrease bone resorption
- promote osteoblast precursor cell recruitment Use:
- osteoporosis - decrease fractures
- hypoparathyroidism
- No kidney/liver activation
Calcitonin (Hypercalcemia, Paget’s)
Effects:
- inhibit osteolysis (decrease serum Ca) and increase Ca excretion
- from salmon or human Use:
- hypercalcemia
- Paget’s
- postmenopausal osteoporosis SE:
- well tolerated
- rash
- vomit
- facial flushing (salmon version b/c of Ab against salmon)
Pamidronate (Hypercalcemia)
Effect:
- bisphosphonate substitute - decrease bone turnover Use:
- hypercalcemia of malignancy
- decrease bone pain/fracture in MM and metastatic breast cancer
- injection; expensive SE:
- Nausea
- anorexia
- leukopenia
- injection site rxn
