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13 Cards in this Set

  • Front
  • Back
Medrol Dose Pak
Class: Corticosteroid
MOA: Alter gene expression to achieve effects; Enter cells and bind to cytosolic receptors, Receptor migrates to nucleus (GR), Binds to response elements (GREs)
Steroid action in inflammation; 2 Mechanisms
1. AP-1and NF-κB; Bind and ↓ actions directly through protein-protein interactions, ↑ expression of glucocorticoid induced leucine zipper proteins (GILZ), High concentrations
2. Chromatin Remodeling;
Anti-inflammatory genes - Acetylation of H4 portion of the histone by steroid co-activator molecules, Anti-inflammatory protein expression
Pro-inflammatory genes - GR binds to pro-inflammatory molecules and inhibits HAT activity, GR recruits histone deacetylases to transcriptional complex
Low concentrations used clinically
Effects: Anti-Inflammatory
Inhibition of; accumulation of macrophages and leukocytes, phagocytosis, lysosomal enzyme release, release of chemical mediators of inflammation
Uses:
Preoperative antimicrobial prophylaxis
Suppression of signs of inflammation

Medrol Dose pack is given in a step down method. “…6 the first day, 5 the second day, 4, 3, you know the rest. That way they’re not going to get into that acute adrenal crisis. This is for something like poison ivy. Or if the pt has an accident with inflammation. If you need to treat someone’s TMJ or trigeminal neuralgia. You might try Medrol dose pack to get rid of the inflammation if other drugs aren’t working.” -KG

Replacement Therapy - most common Prednisone
Indications:
Chronic Inflammatory and Immune Diseases, RA, Lupus, Psoriasis, Crohn’s Disease, Chronic Hepatitis, Asthma, Organ Transplants, TMD, COPD
Do not have any curative properties, decrease signs and symptoms of disease, like inflammation and pain
Adverse:
Withdrawal from Corticosteroids:
Even for short duration therapy (3 days) doses should be tapered
Withdrawal symptoms; Joint pain, Muscle pain, Fatigue, Fever, Nausea and vomiting, Acute Adrenal Crisis Caused by insufficient levels of cortisol; Low BP, Dehydration , Confusion, Tachypnea, Sweating of face and hands, Shock, Coma, Seizures
Fluid and Electrolyte; Sodium and fluid retention, CHF, HTN and potassium loss
Musculoskeletal: Loss of muscle mass, Osteoporosis, Compression fractures
GI; Peptic ulcer, Pancreatitis, Ulcerative esophagitis
Dermatologic; impaired and delayed wound healing, Thin fragile skin,
Neurologic; Convulsions, Vertigo, Headache
Endocrine; Development of Cushing's state, Secondary adrenocortical and pituitary unresponsiveness, Diabetes
Prednisone
Class: Corticosteroid
MOA: Alter gene expression to achieve effects; Enter cells and bind to cytosolic receptors, Receptor migrates to nucleus (GR), Binds to response elements (GREs)
Steroid action in inflammation; 2 Mechanisms
1. AP-1and NF-κB; Bind and ↓ actions directly through protein-protein interactions, ↑ expression of glucocorticoid induced leucine zipper proteins (GILZ), High concentrations
2. Chromatin Remodeling;
Anti-inflammatory genes - Acetylation of H4 portion of the histone by steroid co-activator molecules, Anti-inflammatory protein expression
Pro-inflammatory genes - GR binds to pro-inflammatory molecules and inhibits HAT activity, GR recruits histone deacetylases to transcriptional complex
Low concentrations used clinically
Effects: Anti-Inflammatory
Inhibition of; accumulation of macrophages and leukocytes, phagocytosis, lysosomal enzyme release, release of chemical mediators of inflammation
Uses:
Preoperative antimicrobial prophylaxis
Suppression of signs of inflammation
Replacement Therapy - most common Prednisone
Anti-inflammatory effects only produced by supra-physiologic doses of steroids
7.5 mg Prednisone q Day or more is supra-physiologic dose
Synthetic steroids are less protein-bound = increases active form
increased anti-inflammatory effects
Increased side-effects
Dental Treatment may require a stress dose(pt undergoing siginificant surgical stress and adrenal glands are suppressed so you double daily steroid dose before procedure) of corticosteroid to prevent Acute Adrenal Insufficiency
Indications:
Chronic Inflammatory and Immune Diseases, RA, Lupus, Psoriasis, Crohn’s Disease, Chronic Hepatitis, Asthma, Organ Transplants, TMD, COPD
Do not have any curative properties, decrease signs and symptoms of disease, like inflammation and pain
Adverse:
Withdrawal from Corticosteroids:
Even for short duration therapy (3 days) doses should be tapered
Withdrawal symptoms; Joint pain, Muscle pain, Fatigue, Fever, Nausea and vomiting, Acute Adrenal Crisis Caused by insufficient levels of cortisol; Low BP, Dehydration , Confusion, Tachypnea, Sweating of face and hands, Shock, Coma, Seizures (treatment – 100mg Hydrocortisone IM Trendelenberg, O2)
Fluid and Electrolyte; Sodium and fluid retention, CHF, HTN and potassium loss
Musculoskeletal: Loss of muscle mass, Osteoporosis, Compression fractures
GI; Peptic ulcer, Pancreatitis, Ulcerative esophagitis
Dermatologic; impaired and delayed wound healing, Thin fragile skin,
Neurologic; Convulsions, Vertigo, Headache
Endocrine; Development of Cushing's state, Secondary adrenocortical and pituitary unresponsiveness, Diabetes
Methotrexate
Class: Cytotoxic agent, inhibitor of gene expression
MOA: Folate analog
Anti-inflammatory effects
Apoptosis of CD4 and CD8 T cells
Indications:
Rheumatoid arthritis
Psoriasis
Graft vs host disease
Severe asthma
Effects:
Once a week dosing
Mycophenolic Acid (CellCept)
Class: Cytotoxic agent, Inhibitor of gene expression
MOA: Inhibitor of inosine monophosphate dehydrogenase
Rate limiting enzyme in the biosynthesis of guanosine
Effects: Decreases lymphocyte activation and activity
Induces apoptosis of activated T cells
Decreased expression of adhesion molecules
Decreased production of NO by neutrophils
Oral Adverse Effects: Mouth ulceration, gum hyperplasia, gingivitis, dry mouth, dysphagia
Cyclosporine
Class: Specific lymphocyte signaling inhibitor
MOA:
Inhibits synthesis of IL-2 in activated T-cells
Interleukin-2
Cytokine
Activation and proliferation of T-cells
Nuclear factor of activated T-cells (NFAT)
Has to be dephosphorylated to translocate to nucleus
Dephosphorylated by calcineurin
Form a complex with cyclophilin
Complex binds to calcineurin and inactivates it
Indications: Immunosuppressive for graft survival, Topical for oral lichen planus, Psoriases, RA
Adverse Rxns: Renal toxicity, HTN, Hyperlipidemia, Neurotoxicity, Gingival hyperplasia
Tacrolimus (Prograf)
Class: Specific lymphocyte signaling inhibitor
MOA:
Inhibits synthesis of IL-2 in activated T-cells
Interleukin-2
Cytokine
Activation and proliferation of T-cells
Nuclear factor of activated T-cells (NFAT)
Has to be dephosphorylated to translocate to nucleus
Dephosphorylated by calcineurin
Form a complex with cyclophilin
Complex binds to calcineurin and inactivates it
Indications: Immunosuppressive for graft survival, Topical for oral lichen planus, Psoriases, RA
Adverse Rxns: Renal toxicity, HTN, Hyperlipidemia, Neurotoxicity, Gingival hyperplasia
Diphenhydramine (Benadryl)
Class: Anti-histamine (1st Gen, OTC)
MOA: Inverse agonists at histamine receptor sites - bind to and stabilize the inactive conformation of the H1 receptor, two state model of H1 receptor
Therapeutic Uses: Nasal Allergies, Allergic Dermatoses, Symptomatic relief of the common cold, Sedation
Therapeutic Uses in Dentistry: Allergic lesions of the oral mucosa
Adverse:
CNS depression - drowsiness, lethargy, decreased motor coordination (less than others in same class)
Anti-muscarinic effects - dry mouth, constipation, blurred vision
Meclizine (Antivert)
Class: Anti-histamine (1st Gen, Rx only)
MOA: Inverse agonists at histamine receptor sites - bind to and stabilize the inactive conformation of the H1 receptor, two state model of H1 receptor
Therapeutic Use: Vertigo
Adverse:
CNS depression - drowsiness, lethargy, decreased motor coordination
Anti-muscarinic effects - dry mouth, constipation, blurred vision
Promethazine (Phenergan)
Class: Anti-histamine (1st Gen, Rx only)
MOA: Inverse agonists at histamine receptor sites - bind to and stabilize the inactive conformation of the H1 receptor, two state model of H1 receptor
Therapeutic Use: Nausea
Therapeutic Uses in Dentistry: Reduction of post-operative nausea
Adverse:
CNS depression - drowsiness, lethargy, decreased motor coordination
Anti-muscarinic effects - dry mouth, constipation, blurred vision
Fexofenadine (Allegra)
Class: Anti-histamine (2nd Gen)
MOA: Inverse agonists at histamine receptor sites - bind to and stabilize the inactive conformation of the H1 receptor, two state model of H1 receptorDoes not cross BBB
Therapeutic Uses: Nasal Allergies, Allergic Dermatoses, Symptomatic relief of the common cold, Motion sickness, Sedation
Therapeutic Uses in Dentistry: Conscious sedation, Pre-medication for general anesthesia, Reduction of post-operative nausea, Allergic lesions of the oral mucosa
Adverse:
CNS depression - drowsiness, lethargy, decreased motor coordination
Anti-muscarinic effects - dry mouth, constipation, blurred vision
Loratadine (Claritin)
Class: Anti-histamine (2nd Gen)
MOA: Inverse agonists at histamine receptor sites - bind to and stabilize the inactive conformation of the H1 receptor, two state model of H1 receptorDoes not cross BBB
Therapeutic Uses: Nasal Allergies, Allergic Dermatoses, Symptomatic relief of the common cold
Therapeutic Uses in Dentistry: Allergic lesions of the oral mucosa
Adverse:
CNS depression - drowsiness, lethargy, decreased motor coordination
Anti-muscarinic effects - dry mouth, constipation, blurred vision
Adalimumab (Humira)
Class: Antibody
MOA: Binds to and inactivates tumor necrosis factor α (TNFα)
TNFα: Cytokine, Normal inflammatory and immune responses
Uses: These things are used for psoriasis, Crohn’s disease, rheumatoid arthritis.
Adverse: Headache, rash, nausea
Basiliximab (Simulect)
Class: Antibody
MOA: IL-2 receptor antagonist
IL-2Rα receptor on activated T-lymphocytes
Inhibits IL-2 activation of lymphocytes
Pathway in the cellular immune response
Uses: These things are used for psoriasis, Crohn’s disease, rheumatoid arthritis.
Adverse: Headache, rash, nausea