Naproxen

Indomethacin

 NSAIDs used as co-therapy for acute gout attacks

Indomethacin may cause CNS effects in elderly patients

Aspirin is contraindicated because it may precipitate attacks at low doses

A gout drug made from autumn crocus that inhibits granulocyte infiltration

It inhibits microtubule polymerization, assembly, and neutrophils' ability to migrate to the joint and cause inflammation

Reduces lactic acid production

Prevents elaboration of glycoproteins

Uses: abort acute attacks

Toxicities: mostly GI, aplastic anemia, alopecia, ab pain

Acute poisoning: hemorrhage, GI sx, vascular damage, ascending paralysis, and nephrotoxicity

Admin: oral, IV

Biliary and renal excretion

Not a first choice drug!!

A xanthine oxidase inhibitor pro-drug that reduces the amount of uric acid produced

Metabolized to oxypurinol and alloxanthine, which remain in the system much longer than the drug itself

Decreases plasma uric acid, decreases urine uric acid, decreases xanthine in plasma, dissolves tophi, prevents development of nephropathy

Uses: Prophylactic use in chronic gout to prevent urate deposition, hyperuricemia, prophylaxis for renal calculi

Adverse effects: hypersensitivity rxn, precipiates acute attacks (give with colchicine), fever, malaise, hepatomegaly

Drug interactions: warfarin

Renal clearance

Originally used as anti-cancer agent

Uricosic drug that increases the excretion of uric acid

Breaks down tophi and inhibits tubular reabsorption of uric acid

Used for chronic gout

Adverse effects: GI irritation, hypersensitivity, provokes acute attacks (give with colchicine)

Drug interactions: increases clearance of oxypurinol

Overdoses: CNS effects, coma, death

A glucocorticoid that inhibits mobilization of AA and induces synthesis of lipocortin to inhibit phospholipase A2

Decreases TNF-alpha and cytokines by decreasing NkFB

Increases apoptosis of activated T cells

Used to suppress immune system, inflammation

Used in: graft vs. host, rheumatic disorders, SLE, skin conditions, asthma, allergies, MS

Adverse effects: growth retardation, avascular bone necrosis, osteopenia, infection, cataracts, hyperglycemia, and diabetes when combined with calcineurin inhibitors

A TNF-alpha inhibitor that is used to in combination with MTX in rheumatic syndromes to decrease the rate of formation of bone erosians.

Fusion protein that binds to secreted TNF-alpha and prevents interaction with its receptor to inhibit inflammation.

Adverse effects: reactivates latent TB, infection, increased ANA and dsDNA

Admin: SC 2x per week

NOT effective in UC

A chimeric monoclonal TNF-alpha inhibitor that binds to membrane bound and soluble TNF-alpha to down regulate T cell and macrophage function and reduce inflammation.

Used in: RA, UC, CD in combination with MTX

Adverse effects: may develop Ab after therapy (the risk of this decreases with MTX use), URI, nausea, headache, sinusitis, rash, cough, reactivation of latent TB

Admin: IV every 8 weeks

A T cell activation inhibitor that interferes with co-stimulation of T cells by preventing CD80/86 from binding to CD28. Produces T cell hyporesponsivess, decreased T cell proliferation, decreased cytokines, decreases in all downstream events (B cells)

Used for RA, if other DMARDs have not worked

Adverse effects: serious infections, esp when given with a TNF-alpha inhibitor, lung cancer, lymhoma

Do not give live vaccines

An anti-CD20 monoclonal antibody that selectively depletes CD20 positive B cells to prevent inflammation

Used in RA with MTX, synovitis

Adverse effects: serious infections, viral reactivation, chills, fever, headache, urticaria, bronchospasm, and hypotension

Admin: IV every 2 weeks

Female pts must contraception

An anti-proliferative agent that inhibits DHFR to inhibit thymidine and synthesis of DNA, preventing T cell proliferation

Used for: organ transplants, RA (lower doses), anti-cancer (high doses), arthritis, autoimmune diseases

Adverse effects: nasal and mucosal ulcers, hepatotoxicity, renal damage

Admin: oral or parenteral, absorption is dose dependent

A calcineurin inhibitor that binds to cyclophilin to inactivate NFAT and decrease transcription of IL-2 and cytokine genes to inhibit T cell activatino, proliferation, and differentiation

Used for: transplant rejection, RA, psoriasis, endogenous uveitis, atopic dermatitis, IBD, nephrotic syndrome

Adverse effects: renal dysfunction, tremor, hirsutism, HTN, high lipids, gum hyperplasia, DM when combined with cortisol

Many CYP 3A interactions: Ca channel blockers, antifungals, HIV protease inhibitors, allopurinol, metoclopramide, grapefruit juice, phenytoin, phenobarbital

One of the most effective immunosuppressants

Admin: oral or IV

A calcineurin inhibitor that binds to FKBP to inactivate NFAT and decrease transcription of IL-2 and cytokine genes to inhibit T cell activatino, proliferation, and differentiation

Used for: transplant rejection, RA, psoriasis, endogenous uveitis, atopic dermatitis, IBD, nephrotic syndrome

Adverse effects: renal dysfunction, tremor, hirsutism, HTN, high lipids, gum hyperplasia, DM when combined with cortisol

Many CYP 3A interactions: Ca channel blockers, antifungals, HIV protease inhibitors, allopurinol, metoclopramide, grapefruit juice, phenytoin, phenobarbital

One of the most effective immunosuppressants

Admin: oral or IV

A kinase mTOR inhibitor that inhibits the cell from progressing through the G1 phase of mitosis to inhibit T cell proliferation and activation

Used in organ transplants

Adverse effects: increases cholesterol and TG, increases renal toxicity of cylcosporin, lymphocele, myelosuppression, GI intolerance, fever

Same drug interactions as calcineurin inhibitors

Admin: oral, 62 hour half life

A first line anti-epileptic that increases Na+ channel inactivation.

Used for: partial seizures, GTCs, and status epilepticus

Adverse effects: gingival hyperplasia, hirsutism, cardiac arrhythmias, CNS depression

Admin: oral absorption that is dose dependent

Time to peak varies significantly

Highly bound to proteins, half life 22 hours

Metabolized by microsomal enzymes

A first line anti-epileptic drug that increases Na+ channel inactivation (a tricyclic antidepressant).
Used for: partial seizures, GTCs

Adverse effects: CNS - ataxia, diplopia, nystagmus, dizziness, aplastic anemia, blood dyscrasias, rash

Drug interactions: cimetidine, propoxyphene, diltiazem, erythromycin, isoniazed, verapamil

Produces an active metabolite

A first line anti-epileptic that increases Na+ channel inactivation

Used for: partial seizures, GTCs

Adverse Effects: drowsiness, nystagmus, ataxia

Metabolizes into phenobarbital and phenylethylmalonamide

Half life: 8-12 hours

Not really used in favor of Phenytoin and Carbamazepine

A first line anti-epileptic that increases Na+ channel inactvation

Used for: generalized seizures and absence seizures Also increases GABA levels by inhibiting breakdown

A first line anti-epileptic that inhibits T-type Ca++ channel activity in thalamic neurons

Used for: generalized seizures, absence seizures, myoclonic seizures

Adverse Effects: gastric distress, pain, nausea, vomiting

Not protein bound

Metabolized by microsomal enzymes

Half life: 40 hours

Safter than valproate

A first line benzodiazepine anti-epileptic drug that increases the affinity of GABA for the GABAa receptor

Used for stopping status epilepticus

Prolonged status epilepticus can develop a tolerance to this and other benzodiazepines

Metabolized by microsomal enzymes

A adjunct anti-epileptic drug that binds to voltage gated Ca++ channels to decrease glutamate release

Used for partial seizures with or without secondary generalizations and chronic pain mgmt

Drug Interations: cimetidine, Al and Mg antacids

Originally designed to interfere with the GABAa receptor

An adjunt anti-epileptic drug that increases Na+ inactivation

Used for: partial seizures

Drug interaction: half life reduced by phenytoin, primadone, and carbamazepine

Halfe life prolonged by valproate

Rash

Also inhibits release of excitatory amino acids by acting on presynaptic voltage gated Ca++ channels

An adjunct anti-epileptic that inhibits GABA-T

Used for partial seizures

Adverse effects: psychosis, reduces plasma concentrations of primadone

An adjunct anti-epileptic drug that increases Na+ channel inactivation

Used for partial seizurs and migraines

A beta antagonist that is used as prophylaxis in migraines, mechanism unknown

Adverse effects: fatigue, exercise intolerance, GI disturbances, depression, insomnia, nightmares

Contraindicated in asthmatics

Abrupt withdrawal can cause CV disturbances

A 5HT3 and D2 receptor antagonist used for mild-moderate migraines and particularly helps with nausea because it is an anti-emetic that accelerates gastric emptying

Often used as adjunct migraine therapy since it has a low analgesic effect

A xanthine that blocks phosphodiesterase and causes cerebral vasoconstriction, used for acute mild-moderate migraines. It also potentiates analgesic absorption

Often used as adjunct therapy

An ergot drug, nonselective 5-HT agonist at trigeminal nerves, that is used for acute moderate-severe migraines. It causes cerebral vasoconstriction and is often combined with caffeine and sedatives.

Adverse effects: nausea, cramps, vertigo, cold extremities, gangrene, diarrhea

Can develop a dependence

Contraindicated in pregnancy, sepsis, and vascular disease

It must be taken early in the attack to be effective!

Response is erratic via oral admin

An ergot drug, nonselective 5-HT agonist at trigeminal nerves, that is used for acute moderate-severe migraines. It causes weak cerebral vasoconstriction and is often combined with caffeine and sedatives.

Adverse effects: cramps, vertigo, cold extremities, gangrene, diarrhea

Lesser effect on dependence and nausea

Contraindicated in pregnancy, sepsis, and vascular disease

It must be taken early in the attack to be effective!

Can be given parenterally

A tripan, a derivative of serotonin, that is a very selective agonist at the 5-HT1d receptor used for acute moderate-severe migraines by blocking vasodilation and is the current drug of choice for migraines

Adverse effects: re-emergent migraine is common (withdrawal, or drug wearing off?)

Not many other adverse effects

Use with caution in CAD and avoid use with MAOIs

Many routes of admin: PO, sublingual, IM, nasal

Rapid acting and works after the onset of symptoms