Week 12: Respiratory, Eyes, Ears, and Skin Drugs Flashcards
Characteristics of inflammation (3)
- Increased vascular permeability
- Extravasation of WBC
- Swelling, warmth, redness, pain
Glucocorticoid MoA and effects (3)
MoA:
1. Enter cell via phospholipid bilayer
2. Bind to receptor-steroid complex in cytoplasm
3. Complex moves to the nucleus and binds to chromatin in DNA, altering mRNA transcription
4. Inc. or dec. in protein synthesis
Effects:
- Dec. warmth, redness, pain, and swelling at site of irritation
- Dec. bacterial killing (infection risk)
- Dec. antibody production (dec. humoral immunity)
Cortisone // Hydrocortisone: Class, MoA, AE (9)
Class: Glucocorticoid
MoA: Binds to receptor-steroid complex -> alters mRNA transcription
AE:
- Risk for infection, caution with vaccine administration
- Adrenal insufficiency
- Osteoporosis
- Hyperglycemia
- Growth delay in children
- Fluid/electrolyte disturbances
- Peptic ulcer disease
- Psychological disturbances
- Cataracts and glaucoma
Prednisone: Class, MoA, AE (9)
Class: Glucocorticoid
MoA: Binds to receptor-steroid complex -> alters mRNA transcription
AE:
- Risk for infection, caution with vaccine administration
- Adrenal insufficiency
- Osteoporosis
- Hyperglycemia
- Growth delay in children
- Fluid/electrolyte disturbances
- Peptic ulcer disease
- Psychological disturbances
- Cataracts and glaucoma
Dexamethasone: Class, MoA, AE (9)
Class: Glucocorticoid
MoA: Binds to receptor-steroid complex -> alters mRNA transcription
AE:
- Risk for infection, caution with vaccine administration
- Adrenal insufficiency
- Osteoporosis
- Hyperglycemia
- Growth delay in children
- Fluid/electrolyte disturbances
- Peptic ulcer disease
- Psychological disturbances
- Cataracts and glaucoma
How do exogenous glucocorticoids pose a risk for adrenal suppression?
Long-term therapy suppresses CRH/ACTH due to high glucocorticoid levels =
decreased adrenal synthesis/release of glucocorticoid, resulting in adrenal atrophy
Cyclosporine // Tacrolimus: Class, indications, MoA, AE (10), drug interactions (2)
Class: Calcineurin inhibitors
Indications: Transplant rejection
MoA: Inhibit calcineurin -> suppress IL-2 production = dec. T and B cell proliferation
AE:
- Nephrotoxicity (common)
- Infection (common)
- Hepatotoxicity
- Lymphoma
- Anaphylaxis
- HTN
- Tremor
- Gynecomastia
- HyperK+
- Hyperglycemia
Drug interactions:
- Avoid other nephrotoxic drugs
- CYP450 inducers/inhibitors = organ rejection or drug toxicity
Tacrolimus: What’s unique?
Somewhat more effective than Cyclosporine, but smaller therapeutic index
mTOR inhibitors: Indications, MoA, AE (6)
Indications: Kidney/renal transplant rejection
MoA: Inhibit mTOR = IL-2 inhibition = dec. T and B cell proliferation
AE:
- Infection risk
- HLD
- Myelosuppression -> Anemia, thrombocytopenia, leukopenia
- Nephrotoxicity
Azathioprine // Cyclophosphamide // Methotrexate // Mycophenolate mofetil: Class, MoA, AE (4)
Class: Cytotoxic drugs
MoA: Kills B and T cells that are undergoing proliferation
AE:
- Bone marrow suppression
- GI disturbances
- Reduced fertility
- Alopecia
Azathioprine: What’s unique?
Interferes with folate metabolism
Methotrexate: What’s unique?
Interferes with folate metabolism
Mycophenolate mofetil: What’s unique?
Selective B and T cell inhibition due to suppression of inosine monophosphate dehydrogenase
Antibodies: General MoA and AE (2)
MoA: Directed at components of the immune system = suppressed immune responses
AE:
- High risk for infection
- Hypersensitivities
Actions of H1 receptor agonism (7)
- Vasodilation and inc. capillary permeability (swelling, redness, warmth)
- HypoTN and reflex tachycardia
- Itching and pain (Stimulation of sensory nerves)
- CNS: Cognition, memory, sleep/wake
Diphenhydramine // Promethazine: Class, indications (3), MoA, AE (11), PK
Class: 1st gen H1 receptor antagonists
Indications: Mild allergy or in adjunct in severe allergy
- Motion sickness
- Insomnia
MoA: Selectively blocks H1 receptors
- Some agents can block M receptors (anticholinergic side effects)
AE:
- Sedation
- Dizziness and coordination problems
- Confusion
- Acute toxicity: Hallucination, excitation, seizures (children)
- N/V, loss of appetite
- Constipation
- Dry mouth/eyes
- Dec. DI/GU motility
- Tachycardia
- Respiratory depression at extremes of age
- Avoid use with other CNS depressants
PK: Small, highly lipid-soluble = CNS effects
Fexofenadine: Class, indications (2), MoA, AE (6), PK
Class: 2nd generation H1 receptor antagonists
Indications: Mild allergy or in adjunct in severe allergy
- Motion sickness
MoA: Selectively blocks H1 receptors
- Some agents can block M receptors (anticholinergic side effects)
AE:
- N/V, loss of appetite
- Constipation
- Dry mouth/eyes
- Dec. DI/GU motility
- Tachycardia
- Respiratory depression at extremes of age
PK: Large, polar = no BBB crossing
Asthma: General pathophysiology
Allergen binds IgE antibodies on mast cells
- Release of mediators (histamines)
- Bronchoconstriction + infiltration of inflammatory cells
Chronic bronchitis: Definition and general pathophysiology
33
Emphysema: Definition and general pathophysiology
33
MDI (metered dose inhaler)
36
Respimat
36
DPI (dry powder inhaler)
36
Nebulizers
36
Considerations for bronchodilators (3)
- Bronchodilators don’t alter underlying pathophysiology
- Bronchodilators don’t dec. inflammation
- Most that use bronchodilators must use an anti-inflammatory for long-term management
Albuterol // Terbutaline: Class, indications, MoA, AE (5), administration guidelines (2)
Class: Short-acting B2 agonist (SABA)
Indications: PRN to abort acute attack (acute bronchospasm)
MoA: B2 agonism
AE:
- Tremors
- Tachycardia/dysrhythmia → angina
- Hyperglycemia
- Hypokalemia
- Nervousness
Administration guidelines:
- PO or inhaled
- Also combined with cromolyn to prevent exercise-induced bronchospasm
Salmeterol // Formoterol: Class, indications, MoA, AE (5), administration guidelines (3)
Class: Long-acting B2 agonist (LABA)
Indications: COPD
MoA: B2 agonism
AE:
- Tremors
- Tachycardia/dysrhythmia → angina
- Hyperglycemia
- Hypokalemia
- Nervousness
Administration guidelines:
- PO or inhaled
- Fixed dosing schedule
- Should never be given alone, usually given with glucocorticoid
Theophylline: Class, indications, MoA, AE (5), administration guidelines (2), interactions (4)
Class: Methylxanthine
Indications: COPD
MoA: Block adenosine receptors
AE:
- CNS excitation → seizures
- Cardiac stim → dysrhythmias → cardiac arrest
- Vasodilation → hypotension
- Diuresis
- Nausea/vomiting/diarrhea
Admin guidelines:
- Slow IV admin to avoid fatal CV events
- Monitor plasma levels
Interactions:
- Caffeine → increases AE
- Tobacco/marijuana → induces CYP450
- CYP450 inducers → subtherapeutic theophyline levels
- CYP450 inhibitors → subtherapeutic (toxic) theophyline levels
Ipratropium: Class, indication (1), MoA, AE
Class: Short-acting anticholinergic (SAMA)
Indication: Bronchospasm
MoA: Block M receptors in the bronchi
AE: Quaternary ammonium → minimal AE
Tiotropium: Class, indication (1), MoA, AE
Class: Long-acting anticholinergic (LAMA)
Indication: Long-term bronchospasm prevention
MoA: Block M receptors on bronchi
AE: Quaternary ammonium → minimal AEs
Beclomethasone // Budesonide // Fluticasone: Class, Indication, MoA (3), AE (3)
Class: Inhaled glucocorticoid
Indication: Long-term control of airway inflammation
MoA:
- Decreased synthesis and release of inflammatory factors
- Decreased infiltration of inflammatory cells
- Decreased edema of the airway mucosa
AEs:
- Oropharyngeal candida (thrush)
- Dysphonia (hoarseness)
- Long term high dose therapy can have systemic AE
Zileuton: Class, Administration, Indication, MoA (4), AE (3)
Class: Leukotriene receptor antagonist
Administration: PO
Indication: 2nd line for asthma if pt can’t tolerate glucocorticoids* NOT for acute attack relief
MoA:
- Smooth muscle constriction
- Increased blood vessel permeability
- Increased inflammatory response (directly + through eosinophil recruitment)
- block leukotriene synthesis
AEs:
- Neuropsych effects (depression, SI)
- Liver injury
- CYP450 inhibition
Montelukast: Class (2), Administration, Indication, MoA (4), AE (2)
Class:
- Leukotriene receptor antagonist
- Highly protein bound
Administration: PO
Indication: 2nd line for asthma if patient can’t tolerate glucocorticoids* NOT for acute attack relief
MoA:
- Smooth muscle constriction
- Increased blood vessel permeability
- Increased inflammatory response (directly and through eosinophil recruitment)
- Blocks leukotriene RECEPTORS
AEs:
- Minimal AE
- Rare neuropsych effects
Cromolyn: Class, Indications (3), MoA (3), AE
Class: Mast cell stabilizer
Indications:
- Safest of all anti-asthma drugs
- Exercise induced asthma
- Allergic rhinitis
MoA:
- Decreased histamine and mediator release
- Decreased inflammation
- Does NOT cause bronchodilation
AE: very rare AE
Omalizumab: Class, Indications (2), MoA (2), AEs (4)
Class: Monoclonal antibody IgE antibody antagonist
Indications:
- Not first line drugs; none for acute management
- For serious uncontrolled asthma
MoA:
- Forms complex with IgE that prevents binding
- Decreased inflammatory mediator release
AEs:
- Vital infections
- Injection site reactions → hypersensitivity reactions
- 1/2 life = 26 days, takes 1yr to return to pre-drug levels
- Increased risk of infection for ~1 yr after admin
Monoclonal antibody: Interleukin-5 receptor antagonist: Class, Indications (2), MoA (2), AE (5)
Class: IL-5 receptor antagonist
Indications:
- Not first line drugs; none for acute management
- For serious uncontrolled asthma
MoA:
- Inhibit IL-5
- Decreased eosinophils
AE:
- Headache
- Pharyngitis
- Fatigue
- Hypersensitivity reactions
- Anaphylaxis (RESLIZUMAB)
Monoclonal antibody: Interleukin-4 receptor antagonist: Class, Indications (2), MoA (2), AE (4)
Class: IL-4 receptor alpha antagonist
Indications:
- Not first line drugs; none for acute management
- For serious uncontrolled asthma
MoA:
- Inhibit IL-4
- Decreased cytokine-induced inflammation
AE:
- Injection site reaction
- Oral herpes
- Conjunctivitis
- Antibody development against the drug
Roflumilast: Class, Distinguishing features (2), Indications, MoA (4), AE (6), Contraindication (1)
Class: PDE4 inhibitor
Distinguishing features:
- PO
- 1/2 life 17 hours due to high protein binding
Indication: Severe bronchitis primary COPD (not first line)
MoA:
- Inhibits PDE4
- Increased cAMP
- Suppression of cytokines
- Decrease WBC infiltration
AE:
- Diarrhea
- Anorexia
- Headache
- Back pain
- Insomnia
- Severe psych reactions
Contraindication: avoid in pregnancy
SYMBICORT
Budesonide / Formoterol
ADVAIR
Fluticasone propionate / Salmeterol
COMBIVENT
Albuterol / Ipratropium
Phenylephrine // Pseudoephedrine: Class, Administration, Indication (2), MoA (4), AE (2), Contraindications (1)
Class: Sympathomimetic A1 agonist
Administration: Intranasal
Indication:
- Allergic rhinitis
- Allergic conjunctivitis
MoA:
- A1 agonism in nasal vessels
- Vasoconstriction
- Decreased vascular swelling and permeability
- Effects are rapid and intense
AE:
- CNS stimulation + CV effects at high doses
- Rebound congestion
Contraindications: Can be readily converted into meth
Guiafenesin: Class, MoA
Class: Expectorant
MoA: Promote sputum to expel stuff from lungs
Hypertonic saline // Acetylcysteine (inhaled): Class, MoA
Class: Mucolytics
MoA: Break down thick mucus
Codeine // Hydrocodone: Class, MoA, Distinguishing factors (3)
Class: Opioid antitussive
MoA: Act in CNS to elevate cough threshold
Distinguishing factors:
- Risk for physical dependence is small
- Can still cause respiratory depression
- Formulated with other meds to decrease abuse potential
Dextromethorphan: Class, MoA, Distinguishing factors (2)
Class: Non-opioid antitussive
MoA: CNS actions
Distinguishing factors
- At high doses → euphoria (can be abused)
- NO respiratory depression
Timolol: Class, Administration, Indication, MoA, AE (1)
Class: Beta blocker
Administration: locally (eyedrops)
Indication: Glaucoma
MoA: Decrease aqueous humor production
AE: Systemic beta blockade
Latanoprost: Class, Administration, Indication, MoA (2), AE (1)
Class: Prostaglandin analogs
Administration: locally (eyedrops)
Indication: Glaucoma
MoA:
- Increases AH outflow
- Relaxes ciliary muscle
AE: Ocular hyperemia (enlarged vessels)
Brimonidine: Class, Administration, Indication, MoA, AE (2)
Class: Alpha 2 agonist
Administration: locally (eyedrops)
Indication: Glaucoma
MoA: Decreases AH production
AE:
- Dry mouth
- Ocular hyperemia
Dorzolamide: Class, Administration, Indication, MoA
Class: Carbonic anhydrase inhibitors
Administration: locally (eyedrops)
Indication: Glaucoma (least effective)
MoA: Decreases AH production
Azelastine: Class, Indication, MoA
Class: H1 receptor blocker
Indication: Allergic conjunctivits
MoA: Prevents mast cell activation
Bevicizumab: Class, Administration, Indication, MoA (2)
Class: VEGF inhibitor
Administration: Injected DIRECTLY into vitreous humor
Indication: Age related macular degeneration (WET ONLY)
MoA:
- Prevents VEGF from binding to receptors
- Prevents angiogenesis
Hydrocortisone // cortisone (SKIN): Class, Indication, AE (2)
Class: Topical glucocorticoids
Indication: Rash/itching
AE:
- Local reactions
- Thinning of skin with long-term use
Salicylic acid: Class, Indications (5), AE (1)
Class: Keratoytics
Indications:
- Overgrowth/thickening
- Dandruff
- Psoriasis
- Warts
- Corns
AE: Toxicity with long-term and high-dose use (RARE)
Benzoyl Peroxide: Class, Indication, AE (2)
Class: Topical antibiotics
Indication: Acne (first line)
AE:
- Peeling
- Drying
Tretinoin: Class, Indication, MoA (2), AE (2)
Class: Retinoids
Indication: Acne
MoA:
- Vit A derivatives
- Hyper proliferation of epithelial cells
AE:
- Peeling
- Drying
Methotrexate: Class, Indication, Contraindication (1)
Class: Systemic
Indication: Psoriasis
Contraindication: Pregnancy
Topical tracrolimus: Class, Indication, MoA
Class: Immunosuppressant
Indication: Eczema (2nd line)
MoA: No systemic absorption
Topical minoxidil: Class, Indication, MoA, AE (1)
Class: Direct vasodilator
Indication: Hair loss
MoA: Unknown (maybe increased blood flow)
AE: Local allergic reactions
Amoxicillin: Indication (3)
Indication: Otitis media
- Infants <6m
- 6m-2yr with confirmed disease
- >2y with diagnosis AND severe symptoms
Acetic Acid: Indication (1)
Otitis externa
