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142 Cards in this Set
- Front
- Back
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what is the normal physiology of histamine
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made from histidine
used for growth, neurotransmission stored in mast cells mediator of immune and inflamm. |
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what are the 4 sites that histamine affects
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vascular
neuronal (itching and wakefulness) smooth musc. (bronchoconstriction) exocrine secretion (increases stomach acid, saliva, mucous in lung, etc) |
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what are the targest of the H1 blockers
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CNS (sedatives and antinausea)
drying of mucous membranes PNS (local anesthetic) smooth muscle (dilation) |
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what are the therapeutic indications for H1 antihistamines
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allergic responses
antiemesis, antinausea sedatives |
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what are the 1st gen. H1 antihistamines
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DCCHPT
diphenhydramine clemastine chlorpheniramine hydroxyzine promethazine tripelenamine |
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2nd gen H1 antihistamines
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loren fucks desi's cent
loratadine fexofenadine desloratadine cetirizine |
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toxicity of H1 blockers
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they are CNS depressants so they interact with others like alcohol
"if taking these drugs do not operate heavy machinery" antimuscarinic effects drowsiness |
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what are the H2 blockers
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N.C. ran fam
Nizatidine Cimetidine Ranitidine Famotidine |
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what is unique about the H2 blockers compared to the H1 blockers
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they do not cross into the CNS so they do NOT cause drowsiness...they decrease gastric secretion
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which drug has an anti-androgenic affect (gynecomastic and lower sperm count)
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cimetidine (an H2 blocker antihistamine)
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unique side effect of cimetidine (h2 antihist)
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anti-androgenic (gynecomastic and low sperm count)
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where is serotonin stored
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enterochromaffin cells of the gut
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physiologic effect of serotonin
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smooth muscle constriction (vascular and GI)
itching and pain mood alteration |
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what are the 2 "syndromes" associated with serotonin and how do they differ
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carcinoid syndrome: from a tumor of the enterochromaffin cells which increases 5HT production and causes cramping, bronchospasm, tryptophan deficiency leading to decreasd niacin and pellagra (it is SLOWER)
serotonin syndrome: from taking a serotonin agonist like sumitriptan with an MAO inhibitor which will drastically increase 5HT (it is a RAPID onset) |
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do not take "triptan" drugs with ________ because it may cause ________
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MAO inhibitors; serotonin syndrome
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what drugs can be used to treat migranes
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sumitriptan
ergot alkaloids (partial serotonin agonists) |
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how do the ergot alkaloids work
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used for migraines
partial serotonin agonists also act on NE and DA receptors can cause severe vasospasms leading to gangrene hallucinations |
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s.e.'s of the ergot alkaloids
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severe vasospasms leading to gangrene
hallucinations remember LSD is an ergot alkaloid analog |
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asthma is an ______ disease
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inflammatory
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classes of bronchodilators
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beta 2 receptor agonists
relatively selective b2 agonists cholinergic blockers PDE inhibitors |
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beta 2 receptor agonists
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epi
isoproterenol (both b1 and b2 effects) |
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which b2 receptor agonist is not used to treat asthma usually because it had both b1 and b2 effects?
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isoproterenol
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what is used for anaphalactic shock
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epi
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relatively selective b2 agonists
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"rols and nols" + terbutaline + isoetharine
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which 3 relatively selective b2 agonists have a long duration of action
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FAS
formoterol arformoterol salmeterol |
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side effects of b2 agonists
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tachycardia
muscle tremor (because there are some b2 receptors in skeletal muscle) |
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what cholinergic blockers are used to treat asthma
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ipratropium
tiotropium they are less effective and slower than b2 agonists and they cause dry mouth and dilated pupils (b/c they are muscarinic blockers) |
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which PDE inhibitor is used to treat asthma
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theophylline
(like caffeine) increased CNS increased CV |
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what classes of anti-inflamm. agents can be used to treat asthma
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mast cell inhibitors (cromoln sodium and nedocromilin)
glucocorticoids (sone, lone, olide, onide) anti IgE antibody (omalizumab) inhibitor of LT synthesis (zileuton) LT receptor blockers ("lukast") |
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how does cromolyn sodium and nedocromolin work
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inhibit release of mediators from mast cells (used for asthma)
can cause: cough, throat irritation, bad taste |
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what is the DOC for prophylaxis of asthma
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inhaled glucocorticoids
(sone, lone, sonide, solide) |
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which drug inhibits the synthesis of LT's by inhibiting the enzyme 5 lipoxygenase
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zileuton
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side effects of zileuton
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hepatic inflamm.
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which drugs block LT receptors
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"lukast"
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what are the 4 general physiologic effects of NSAIDS
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analgesic
antipyretic anti-inflamm anti-platelet (dec. clotting) |
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aspirin is a weak ______ so it is absorbed in the ______
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acid; stomach
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aspirin inhibits_______
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COX 1 and COX 2
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do not give ASA to kids. why?
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can cause Reyes syndrome (so don't give ASA to kids that have a viral fever)
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how does ASA work as an anti-clotting agent?
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it inhibits productions of TXA2
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what are the most common side effects of ASA and what do you give for it
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GI effects; give misoprostol but it CAUSES ABORTION!!!
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side effects of ASA
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GI (can give misoprostol but that causes abortion)
tinnitus decreased kidney perfusion hypersensitivity (Reye's in kids) decreased uterine contractions |
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what is unique about acetaminophen
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it has NO anti-inflamm. effects so it cannot be used for RA for example
OD can lead to LIVER damage...due to decr. SH reducing equivalents...give N-acetyl-cysteine |
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what do you give to treat liver damage from tylenol
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n-acetyl-cysteine or any other compound with SH groups
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what are the differenent classes of NSAIDs
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propionic acid derivatives
acetic acid derivatives other |
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what are the propionic acid derivatives NSAIDs
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"pro" ....profen, proxyn, prozin
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what are the acetic acid derivatives NSAIDs
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ITS
indomethacin...potent COX inhibitor to close patent ductus arteriosus tolmetin sulindac |
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"other" NSAIDs
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"fenac"
"dolac" pyroxicam nabumetone |
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what is a COX 2 inhib and why don't we used them
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celecoxib...CV side effects like stroke, MI (too much vasoconstriction)
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glucocorticoids are all derived from
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cholesterol
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deficiency in cortisol
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addison's
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excess cortisol
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cushing's
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what is one protein that glucocorticoids induce and what happens
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lipocortin-1...it inhibits phospholipase A2 and COX2....decreased PG, LT, and cytokines......profound suppression of immune cells
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which glucocorticoids are prodrugs
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cortisone and prednisone
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short acting glucocorticoids
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cortisone
hydrocortisone |
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intermediate acting glucocorticoids
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PTP
prednisone triamcinolone prednisolone |
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long acting glucocorticoids
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"methasones"
dexamethasone betamethasone |
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side effects of glucocorticoids
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adrenal suppression (taper off the dose)
metabolic effect cataracts, glaucoma skin peptic ulcer CNS mood alteration increased susceptibility to infection CV effects |
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why are inhaled glucocorticoids used to treat asthma
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(they are the prophylactic DOC)
b/c they are inhaled they go straight to the lung and cause fewer side effects |
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what is a rabbit polyclonal antibody used against human T cells
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atgam
antithymocyte globulin |
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which monoclonal ab can cause a first dose effect (huge number of cytokines released leading do flu like symptoms or life threatening fever)
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muromonab or orthoclone
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what can you do to prevent the first dose effect caused by muromonab
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give a pretreatment of glucocorticoids to decrease cytokine production to prevent the flu like symptoms and fever
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what binds to cd2 and what does it treat
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alefacept
psoriasis |
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what binds to cd11a and what does it treat
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efalizumab
psoriasis |
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why does muromonab cause the first dose effect
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b/c it is a MOUSE mAb
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what does muromonab treat
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acute renal transplant rejection
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what does etanercept treat and how does it work
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RA
binds to TNF |
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infliximab
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binds TNF
RA and crohns |
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adalimumab
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binds TNF
RA |
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certolizumab
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binds TNF
RA and crohns |
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golimumab
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binds TNF
RA |
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which ones bind TNF
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I.C.A.G.E.
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IL 1 blockers
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anakinra...il1 receptor blocker (RA)
rilonocept...binds il1 (RA) |
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what does cyclosporine treat
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transplantation
dry eye |
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how does cyclosporine work
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binds to a protein cyclophylin then the complex inhibits calcineurin which inhibits NFAT which inhibts gene activation
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side effects of cyclosporine
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nephrotoxicity (major one)
cosmetic: hypertrichosis, gingival hyperplasia |
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which drug causes nephrotoxicity, hypertrichosis, and gingival hyperplasia
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cyclosporine
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how does tacrolimus work
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binds to FKBP and this complex inhibits calcineurin
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side effects of tacrolimus
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nephrotoxicity
hair loss DIABETES |
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which drug can cause diabetes
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tacrolimus
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how does sirolimus work
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binds to FKBP and ultimately inhibits IL-2 induced gene transcription
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what do you use with sirolimus
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tacrolimus or cyclsporine+glucocorticoids
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side effect of sirolimus
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decreased WBCs
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daclizumab
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inhibits il2 receptor
used w/ cyclosporine |
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basiliximab
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inhibits il2 receptor
more ANTIGENIC than daclizumab used with cyclosporine |
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azathioprine
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inhibits t cell replication
prodrug...converted to 6 MP inhibits guanosine (purine) synthesis BONE MARROW SUPPRESSION |
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which drug can cause bone marrow suppression leading to leukopenia, megaloblastic anemia, and thrombocytopenia
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azathioprine
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mycophenolate mofetil
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more specific replacement for azathioprine
prodrug...metabolized into MPA which inhibits IMP dehydrog which is necessary for purine synthesis (so it inhibits purine synthesis) |
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which drugs inhibit purine synthesis
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azathioprine (6-mercaptopurine)
mycophenolate mofetil |
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what is the drug of choice for RA
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methotrexate
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how does methotrexate work
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inhibits dihydrofolate reductase which inhibits the formation of tetrahydrofolate which is needed for essential cell components
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methotrexate is an inhibitor of all cells that________
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turn over rapidly (gi, hair, skin, etc)
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which drug inhibits pyrimidine synthesis
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leflunomide
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how does leflunomide work
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inhibits dihydro-orotate dehydrogenase which is needed for pyrimidine synthesis (so it inhibits pyrimidine synthesis)
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which drug can cause fetal damage
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leflunomide
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major side effect of leflunomide
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fetal damage...if you want to have a kid you take a bile acid binding resin to remove leflunomide from your system
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hydroxychloroquine
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in macrophage
interferes with antigen processing used for RA se: irreversible retinal damage |
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which drug can cause irreversible retinal damage (blindness)
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hydroxychloroquine (the macrophage inhibitor)
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how does abatacept work
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binds to CD80
for RA |
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what binds to CD80
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abatacept
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what does abatacept treat
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RA
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what drug treats MS
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natalizumab
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how does natalizumab work
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binds to integrin receptor on t cell
treats MS |
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what binds to il6 receptors
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toclizumab
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what does toclizumb treat
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RA
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what binds to il12 and il23 and what does it treat
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ustekinumab
psoriasis |
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what are the classes of non-specific cancer drugs
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alkylating agents
antibiotics |
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what are the classes of specific cell cycle cancer drugs
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antimetabolites
mitotic spindle inhib enzyme inhib |
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what are the classes of newer agents of cancer drugs
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kinase inhib
monoclonal ab's proteosome inhib |
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what are the alkylating agents for cancer and how do they work
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cyclophosphamide
lomustine add an alkyl group to the DNA which causes it to cross link |
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Too little cortisol is called what?
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adrenal insufficiency- Addisons
1' High ACTH POMC-->MSH 2' Low ACTH no hyperkalemia just cortisol 3' Abrupt stop of corticosteroids |
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which drug causes eye and ear toxicity
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cisplatin
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what are the antibiotics used for cancer
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doxorubicin...free radicals, heart damage
dactinomycin bleomycin...pulmonary fibrosis all of these intercalate with DNA |
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what are the antimetabolites used for cancer
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folate antagonist: methotrexate
pyrimidine analog: 5FU purine analog: 6-MP |
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what can be given with methotrexate to help prevent some of the toxic effects like immunosuppression
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leucovorin
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what is leucovorin used for
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it can be given with methotrexate to prevent some of the toxic effects
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how does 5 FU work for cancer
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inhibits thymidylate synthase (inhibits pyrimidine synthesis)
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how does 6 MP work for cancer
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inhibits enzymes needed for purine synthesis (remember azathioprine is converted to 6 MP)
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what are the plant alkaloids used for cancer
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vincristine/vinblastine...bind microtubules
paclitaxel...abnormal microtubules etoposide...inhibits topoisomerase 2 topotecan...inhibit topoisomerase1 |
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how does vincristine/vinblastine work
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bind to and inhibit microtubules
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how does paclitaxel work
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forms abnormal MT's
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which drugs inhibit topoisomerase 1 and 2
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etoposide...inhibits topoisomerase 2
topotecan...inhibits topoisomerase1 |
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which drug for prostate tumors
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flutamide
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how does flutamide work
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anti-androgen; inhibits movement of the androgen-androgen receptor complex to the nucleus
for prostate tumors |
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tamoxifen treats
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breast cancer
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how does tamoxifen work
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blocks estrogen receptor
s.e.=retinal damage and cataracts |
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side effects of tamoxifen
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EYE DAMAGE (retinal damage and cataracts)
tammy has bad eyes |
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what does anastrozole treat
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breast cancer
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how does anastrozole work
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inhibits aromatase (so inhibits estrogen synthesis)
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what cancers does prednisone treat
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immune cell dependent cancers like leukemias and lymphomas
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what is used to treat CML
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imitinib
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how does imitinib work
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it is a kinase inhibitor and it allows cells to die (in CML there is usually a protein that stops apoptosis and imitinib inhibits this and allows the cell to die)
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what does geftinib do
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it is a tyrosine kinase inhibitor that blocks EGF-R
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kinase inhibitors
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"inib"
*they end in "ib" for inhibitor they are specific for cancer cells |
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which drugs are specific for cancer cells
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kinase inhibitors...'inib"
proteasome inhibitor...bortezomib trastuzumab bevacizumab rituximab |
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how does bortezomib work
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it is a proteosome inhibitor...by inhibiting proteosomes, the cell cannot remove all the extra "stuff" so the cells die
it contains boron used to treat multiple myeloma |
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what is used to treat multiple myeloma
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bortezomib (proteasome inhibitor)
"bort has multiple proteasomes" |
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what monoclonal ab's are used for cancer
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TBR..."trash be right"
trastuzumab...HER2...breast bevacizumab...VEGF...colon rituximab...CD20 on B cells...lymphomas and leukemias |
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what drugs can be used for breast cancer
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"TAT"
tamoxifen...estrogen receptor anastrozole...aromatase trastuzumab...HER2 |
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what is used for colon cancer (also lung and breast)
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bevacizumab
directed against VEGF so tumors cant get blood supply |
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how does bevacizumab work
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directed against VEGF so tumors can't get blood supply
for colon cancer (and lung and breast) |
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how does rituximab work
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directed against CD20 on B cells
for lymphomas and leukemias |
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difficulties in treating neoplasia
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many drugs inhibit rapidly dividing cells and not all cancers are rapidly dividing
normal cells can be affected not all cancer cells are killed by treatment cancer cells may become resistant to the drugs some drugs may not enter CNS so difficult to treat CNS tumors drugs may cause DNA damage which may lead to other cancers |
