Pharm rheum review

Partial agonist/antagonist at Alpha 1 and Serotonin receptors.
Vasoconstriction. Vasoconstriction early in migraine is useful.
Uterine contraction: used postpartum to control bleeding.
Diagnosis of variant angina, finds reactive coronary segments.

Ergotamine, Ergonovine
, Dihydroergotamine Toxicity

Nesiritide

Bimatoprost

Travoprost

Unoprostone

Bind or block CD20, CD28 or CD80 receptors on T-Cell, B-Cell and APC Cell

causes vasoconstriction used to treat migraine. Can be used as anxiolytic, long onset and duration.

blocks T and B-Cell proliferation. inhibits purine synthesis. not Azathioprine

initiates a complement reaction which stimulates phagocytosis

binds IL-2 receptors on activated T-Cells.

Ocular Side Effects of Latanoprost

combined with misoprostol to induce labor.

Used to treat rheumatic fever and Kawasaki dz

increases hypothalamus set point – hyperthermia, fever.

“Displacement reactions” –warfarin, heparin, phenytoin and sulfonylureas.
Decreases clearance of methotrexate ~severe toxicity.
Phenobarbital induces its metabolism.
Antacids decrease its absorption.
Alcohol/corticosteroids will increase its GI effects.

Diclofenac

Phenylacetic acid derivative; COX-1=COX-2GI ulceration is less frequent; especially in combination with omeprazole or misoprostol. Highest incidence for renal effects (impair blood flow and glomerular filtration rate). Opthalmic preparation for postoperative opthalamic inflammation. Topical gel for solar keratoses. Rectal suppository: postoperative nausea.

Nonselective COX inhibitor
Derived from salicylic acid but not metabolized to salicylic acid or salicylate. Enterohepatic circulation, with reabsorption of its glucuronide metabolite. Cleavage of glucuronide will release the active moiety. RA treatmt. Effective for dental pain (third molar extraction).

Propionic acid derivative; COX-1=COX-2. Reduction of tumor necrosis factor alpha (TNFα). Extensive hepatic metabolism but no enterohepatic circulation. Opthalmic preparation (stops intraoperative miosis). IV. Gynecologic. Rarely causes ataxia, tremor, and cogwheel rigidity (Parkinson-like effect)

Phenylpropionic acid derivative; COX-1=COX-2. Closes ductus arteriosus in preterm infants. Effective in reducing fever in children > 102°. Antagonizes platelet inhibition when given concurrently with lo-dose aspirin. Holds true for most NSAIDS.

Propionic acid derivative; nonselective COX inhibitor and lipoxygenase. However, not superior to any other NSAID. Probenecid elevates its levels and t1/2. Produces fluid retention.

Has NSAID properties but used mainly as an analgesic. May replace morphine in certain situations of postsurgical pain. Can decrease opioid requirement. IM, IV, po, and opthalmic. Renal toxicity (limit to 7 day use).

Osteoarthritis, RA, and acute painInhibits COX-2 > COX-1, thus producing less GI effects than other NSAIDs. Rash

Only nonacid NSAID; converted to acetic acid, prodrugt1/2 24h; daily dosing; renal impairment doubles t ½. Less damage to GI. High doses needed; expensive. Photosensitivity

Naphthylpropionic acid derivative. SR formula, oral suspension, topical, and opthalmic formulas. Rare cases of allergic pneuminitis, leukocytoclastic vasculitis, and pseudoporphyria reported. COX-1=COX-2

Propionic acid derivative; very long t1/2 (60 h). Daily dosing. Lowers serum uric acid; great for GOUT.

Oxicam; at high conc inhibits PMN leukocyte migration, decr O2 radical production, and inhibits lymphocyte function. Long t ½ (daily dosing)
Very high risk of GI bleed at high dose, especially in the elderly. COX-1>COX-2

Sulfoxide prodrug; enterohepatic cycling. An active sulfide metabolite is excreted in bile and reabsorbed. Prolongs duration of action. Suppresses familial intestinal polyposis- inhibits colon cancer development. Steven Johnsons Syndrome, agranulocytosis, and nephrotic syndrome. May elevate aminotransferases

Have more adverse effects than NSAIDs w/o any superiority, inaddition to more GI effects. Diarrhea, Decr in hematocrit or Hb can occur w/ meclofenamic acid.
Meclofenamic acid -for primary dysmenorrhea but therapy should not go past one week.
Meclofenamate sodium- RA and osteoarthritis

For primary dysmenorrhea but therapy should not go past 1 week. Fenamate type drugs. NSAID

treats RA & osteoarthritis. NSAID. Fenamate type drugs.

NSAID w/ greatest toxicity

NSAID w/ high GI & renal effects

NSAID w/ higher liver fxn test abnormalities

Related to piroxicam in structure. Considered “preferentially” COX-2 selective rather than “highly”selective like celecoxib. Approved for osteoarthritis in the U.S.

effects of cortisol deficiency

Use of corticosteroids in neoplastic dz

corticosteroid most commonly leading to withdrawal

Lymphoma risk is incr in which RA med?

hydroxychloroquine adverse effects

adverse effects of cyclophosphamides

adverse effects of cyclosporine

Sulfasalazine MOA (anti RA)

Sulfasalazine adverse effects

inhibits dihydroorotate dehydrogenase, leading to a decrease in ribonucleotide synthesis and arrest at the G1 phase. “Pyrimidine
synthesis inhibitor”. Inhibits T-cell proliferation and production of autoantibodies by B cells. Decreases TNF-α-dependent NF-ĸβ activation.

adverse effects of Leflunomide

Abatacept

Rituximab

Infliximab Adverse Effects

Adverse effects of Adalimumab

adverse effects of Entanercept

adverse effects of Abatacept

adverse effects of Rituximab

Tricyclic Antidepressants (TCA): Imipramine NE, 5-HT, Amitriptyline NE, 5-HT

side effects of tricyclic antidepressants

Phenelzine (irreversible) & Tranylcypromine (reversible)

Selegiline & Rasagiline

Side effects of Phenelzine & Tranylcypromine

side effects of Selegiline and Rasagiline

Fluoxetine (Prozac), Paroxetine (Paxil), Sertraline (Zoloft), Citalopram (Celexa)

side effects of SSRI's

5-HT2 antagonist (also H1 and M3 antagonist)

DA-2 antagonist (also H1, M3, 5-HT2, Alpha-1 block)

Usefulness: Allergic rxns, Hay fever, Nightmares, Serotonin Syndrome, Carcinoid
Side Effects: Dizziness, Drowsiness (H1), Blurred vision, Constipation, Dry mouth (M3)

Usefulness: Antipsychotic (DA antagonist), Schizophrenia, Manic phase bipolar disorder, Severe N/V (anticholinergic)
Side Effects: Constipation, sedation, dry mouth, urinary retention (anti-Ach), Hypotension (Alpha-1 antagonist), Akathisia, dystonia, tardive dyskinesia (DA antagonist)

Structural pre-Prozac (fluoxetine)

Blocks T-cell proliferation. Acts downstream of IL-2 receptor. Inhibits cell cycle at the G1 to S Phase
Toxicity: Hyperlipidemia, Anemia, Potentiates cyclosporine nephrotox.

Blocks T and B Cell proliferation. Blocks purine synthesis and salvage pathways needed for replication. 6-MP

Toxic for rapid growth cells, Leukopenia Thrombocytopenia, GI Ulceration, Hepatotoxicity, Risk of infection
Reduce dose w/ allopurinol (inhibits xanthine oxidase, metabolism of 6-MP)

Blocks T and B Cell proliferation.Inhibits de novo purine synthesis
Toxicity: Same as Azothioprine, minus allopurinol drug-drug interaction. No 6-MP

GI: mucositis, stomatitis, N/V, diarrhea
Blood: 7-10 days following dose, leukopenia and thrombocytopenia with recovery at 2 weeks. Possible pancytopenia at 2 weeks.
Liver: Mild to mod. Hepatits
CNS: Intrathecal admin. – seizures
Pregnancy: Embryotoxic, teratogenic
Renal toxicity

Alkylating agent that blocks DNA replication. Toxicity: Same as Azothioprine, minus allopurinol drug-drug interaction. No 6-MP. Leukopenia, thrombocytopenia, liver toxicity, infection, ulceration

Destruction of lymphocytes by complement activation and phagocytosis.
Toxicity: Fever, Hypotension, Type III hypersensitivity reaction

Ab that Binds to IL-2 receptors on activated T-cells
Toxicity: Potential for anaphylactoid reactions