RA meds Flashcards
What is the cellular cause of RA? What type of hypersensitivity is this?
T cell activation
Also, immune factor stage
What are the three stages of RA?
Initiation stage
Amplification
Final stage (chronic inflammation)
What is the antibody that is elevated in RA? What is this?
Rheumatoid factor
IgM to the Fc of IgG
What are the chemokines that are released in RA? What do these cause?
TNF-a
IL1
IL6
Inflammation and fibrosis
What is the first line treatment for RA?
NSAIDs (ASA, acetaminophen, indomethacin, IBU etc)
What is the role of glucocorticoids in RA?
Reduce the inflammation and cause dramatic improvement in RA
What are the disease -modifying anti-rheumatic drugs (DMARDs)? MOA?
Drugs that reduce inflammation, improve symptoms, and slow bone damage
MOA unknown
Do NSAIDs affect the course of RA? What about DMARDs?
No for NSAIDs
Yes for DMARDs
What is the timeframe of onset for DMARDs?
slow (6 weeks to 6 months)
What are the two different DMARDs?
Synthetic and biologic
What is the MOA of methotrexate? What is the effect in RA treatment?
Inhibits AICAR transformylase to increase extracellular adenosine and inhibit T cell activation
First line treatment for RA
What is the MOA of cyclosporin?
Inhibits IL1 and IL2 receptor production
What is the MOA of cyclophosphamide?
Crosslinks DNA to prevent cell replication
What is the MOA of azathioprine?
Interferes with nucleic acid metabolism and synthesis, and inhibits cell proliferation
Suppressed B and T cell function
What is the MOA of Leflunomide? What is its role in RA treatment?
Inhibits ribonucleotide synthesis and causes cell cycle arrest
First agent for RA
What are the antimalarial agents that are used to treat RA? MOA?
Chloroquine and hydroxychloroquine
MOA unknown
What are the biological DMARDs?
Organic compounds made by living cells modify biologic responses
What are the two drugs that are anti-TNF-a antibodies?
Etanercept
Infliximab
What is the MOA of rituximab?
B cell depleting agent
What is the MOA of abatacept?
T-cell costimulation inhibitor
What is the MOA of Anakinra?
IL-1 cytokine inhibitor
What is the MOA of Etanercept?
anti-TNF-a antibodies
What is the MOA of Infliximab?
anti-TNF-a antibodies
What is the definition of a migraine?
HA from 4-72 hours
Is: unilateral, pulsating, moderate-severe pain
Associated with N/v
What are the characteristics of migraine headaches (location, quality, severity, aggravating factors,)?
Unilateral
Pulsating quality
Aggregated by physical activity
Which gender is more commonly affected with migraines?
Women
What two parts of the head anatomy are affected with migraine HAs?
Dural vasculature
CN V dysfunction
What happens to the blood vessels in migraine headaches?
Vasodilation in the brain, causes stimulation of the mechanoreceptors in the trigeminal nerve, causing ssx.
What are the temporal progression of migraine headaches?
- Premonitory phase
- Aura
- HA
- Resolution
- Postdrome
What are the ssx of the postdrome phase of migraine HAs?
Hangover, fatigue
What happens to the cerebral blood flow with the progression of a migraine HA?
Lower in aura phase, then big increase in HA phase
What are the three main specific migraine treatments?
Ergotamine
Dihydroergotamine
Triptans
Who are the candidates for preventative therapy for migraines?
Unresponsive to acute attack meds
Frequent attacks
What are the two beta blockers that are used in migraine headaches?
Propranolol (beta 1 and 2)
Metoprolol (beta 1)
What is Amitriptyline?
TCA antidepressant
What are the two anticonvulsants used to treat migraine HAs?
Valproic acid
Topiramate
What is the MOA of valproic acid?
GABA-A receptor agonist
What is the MOA of Topiramate?
GABA-A receptor agonist
What is the MOA of Verapamil?
CCB
What is the side effect of overuse of NSAIDs for the treatment of migraines?
Can transform migraine into a more severe, chronic disorder
What type of drug is meperidine? What drug should this never be used with?
Opiate analgesic
What type of drug is butorphanol?
Opiate analgesic
What are the antiemetics that are used for migraine HAs?
Metoclopramide
Chlorpromazine
Prochlorperazine
What is the MOA of Metoclopramide?
weak 5HT3 receptor antagonist
What is the MOA of Chlorpromazine?
Centrally acting D2 receptor antagonist
What is the MOA of Prochlorperazine?
Centrally acting D2 receptor antagonist
What are the two ergot derivatives?
Ergotamine
Dihydroergotamine
What is the MOA of ergot derivatives? What are these used for?
Vasoconstriction d/t stimulation of alpha adrenergic and 5HT 1D receptors
Used for Acute migraines
What are the disadvantages of ergot derivatives?
Complex pharmacology and pharmacokinetics
Potent and sustained vasoconstrictive effect
What is the MOA of sumatriptan (and other Triptans)? What does this cause? What are these used for?
Selective 5HT 1D and 1B receptor agonists used in the treatment of migraine HAs
Inhibit nociception of CN V, cause cranial vasoconstriction
Why are the triptans better to treat migraine HAs over ergot derivatives?
More selective pharmacology
Safer
What is the ultimate treatment for migraine headaches?
Sleep
What is the major adverse effect of triptans?
Agina
MI (Rarely)