Pharmacology 2 Flashcards

Question

Pharmacokinetics of basiliximab

Answer 1

Supplied as a lyophylized powder that is reconstituted for IV administration 20 mg is given IV as a bolus injection or as an infusion over 20-30 min First 20 mg dose is given 2 hr prior to surgery Second 20 mg dose is given 4 days after transplantation Elimination half-life is ca. 7 days; normal T cell numbers return in 7-14 days

Answer 2

``` Incidence and severity much lower than muromonab-CD3 GI (10%): NVD, pain MET: electrolyte imbalances (3-10%) CV (3-10%): hypertension, arrhythmias Rare, potentially fatal anaphylaxis ``` Pediatric patients

Answer 3

Fully humanized monoclonal antibody Immunosuppressive human IgG vs. TNF-a TX for rheumatoid arthritis, Crohn’s disease, ankylosing spondylitis, psoriasis

Answer 4

Binds to TNF-a, preventing its interactions with p55 and p75 cell surface TNF receptors; decreases biological activity of TNF-a Clinical response is ↓ levels of pro-inflammatory cytokines such as IL-1 and IL-6, ↓ leukocyte migration, ↓ activation of neutrophils and eosinophils, ↓ fibroblast proliferation, ↓ synthesis of prostaglandins, ↓ matrix metalloproteinases that produce tissue remodeling responsible for cartilage destruction

Answer 5

Supplied in prefilled syringes containing 20 mg or 40 mg for SC injection Usual maintenance dose is 40 mg Q 2 weeks Elimination half-life is 10-20 days (mean ca. 14 days)

Answer 6

``` Mild injection site reactions Headache (12%) Rash (12%) CV: hypertension (5%) MET: hyperlipidemia (6-7%) ``` Chronic or recurrent infection; tuberculosis Travel to regions where mycoses or tuberculosis are endemic

Answer 7

Prodrug; semisynthetic derivative of mycophenolic acid obtained from Penicillium species Used concomitantly with or as an alternative to cyclosporine or tacrolimus to prevent organ rejection after renal, cardiac, or liver transplants; recommendation is mycophenolate mofetil + cyclosporine + corticosteroid Less bone marrow suppression than azathioprine

Answer 8

Mycophenolic acid is a reversible inhibitor of inosine monophosphate dehydrogenase, inhibits the de novo pathway of guanosine biosynthesis that is critical to lymphocyte proliferation and activation, resulting in blunted T and B cell responses Selective for lymphocytes; other cells are able to recover purines via a separate salvage pathway and are thus able to escape the effect

Answer 9

Supplied as PO and IV formulations; both routes offer essentially complete bioavailability of mycophenolic acid Usual dose is 1 g BID for kidney and liver transplants, 1.5 g BID for heart transplants The inactive phenolic glucuronide is the main metabolite; excreted almost entirely in the urine

Answer 10

``` GI: NVD (13-36%), abdominal pain CNS: headache (16-54%) CV: hypertension (28-77%) HEM: myelosuppression (9-35%) DERM: acne (10%) rash (8%) ``` Chronic renal insufficiency, pregnancy category D

Answer 11

dilates pupil, inhibits saliva flow, accelerates heart rate, dilates bronchi, inhibits peristalsis and secretion, conversion of glycogen to glucose, secretion of adrenaline and noradrenaline, inhibits bladder contractions.

Answer 12

constricts pupil, stimulates saliva flow, slows HR, constricts bronchi, stimulates peristalsis and secretion, stimulates release of bile, contracts bladder.

Answer 13

Choline gets acetylated by choline-acetyl transferase using the acetyl group from acetylCoA

Answer 14

Permanent positive charge on acetylcholine, so doesn't last long if not in vesicles. Hydrolyzed by acetylcholine esterase back to an acetyl group and choline.

Answer 15

Starts w/ tyrosine--> dihydroxyphenylalanine (DOPA) via tyrosine hydroxylase adding an –OH to the 5 C on the ring. DOPA then converted to DA via action of aromatic amino acid decarboxylase that removes the COOH moiety on the side chain. DA converted to NE by dopamine beta hydroxylase that adds an –OH to beta position of the side chain. This occurs inside the vesicle. NE gets converted to E via phenylethanolamine-N-methyltransferase that adds methyl group to the NH on the side chain.

Answer 16

Dopamine metabolism: via MAO and aldehyde DH to convert to DOPAC, then COMT converts to HVA by methylation of a catecholhydroxylation. Another pathway uses COMT to give 3-methoxytyramine, then MAO and ALDH to give HVA. NE and E metabolism: all ends up as VMA, excreted in urine and measured as marker for NE and E funct. If NE and E metabolized by MAO and ALDH first, give dihydroxymandelic acid, then COMT to VMA. If NE by COMT first, give normetanephrine then metabolized by MAO/ALDH to VMA. E w/ COMT first give metanephrine, then metabolized by MAO/ALDH to VMA.

Answer 17

Gs prot incr cAMP via activation of adenyl cyclase, activating PKA to phosphorylated Ca++ channels that increase Ca++ influx leading to incr HR at SA node, incr conduction velocity at AV node, and incr force of contraction at myocardium.

Answer 18

Synthetic carbamoyl ester of choline Main uses are for obtaining miosis during surgery and for reducing IOP elevation in the initial 24 hr following cataract surgery

Answer 19

Agonist at muscarinic receptors; significant NN activity | Constricts the iris and ciliary body resulting in reduction in IOP

Answer 20

Supplied as a 0.01% solution that is instilled into the anterior chamber of the eye Miosis is usually maximal within 2-5 min after administration Not susceptible to AChE inactivation Duration of miosis ~ 24 hr

Answer 21

Rarely iritis or corneal clouding ``` Acute cardiac failure; bradycardia Asthma Hyperthyroidism Peptic ulcer Urinary tract obstruction Parkinsonism ```

Answer 22

Synthetic acetylcholine analog | Indicated for the diagnosis of airway hyperreactivity

Answer 23

Agonist at muscarinic receptors; slight nicotinic activity

Answer 24

Supplied as a lyophilized powder that is reconstituted in isotonic saline for inhalation via nebulizer Three-fold more resistant to AChE than acetylcholine Most subjects return to baseline pulmonary function after 30-45 min

Answer 25

Headache Throat irritation Lightheadedness Itching ``` Acute cardiac failure; bradycardia Asthma Hyperthyroidism Peptic ulcer Urinary tract obstruction ```

Answer 26

Synthetic acetylcholine analog DOC for promoting GI and urinary bladder motility for postop and postpartum nonobstructive urinary retention, neurogenic atony of the urinary bladder, and postop gastric atony or gastroparesis

Answer 27

Muscarinic agonist with no nicotinic activity

Answer 28

Available as tablets for PO dosing, usually 10-50 mg TID-QID Onset occurs in 60-90 min and duration is usually 60 min Not susceptible to AChE inactivation

Answer 29

Rare, but reflect cholinergic stimulation ``` Acute cardiac failure; bradycardia Asthma Hyperthyroidism Peptic ulcer Urinary tract obstruction Parkinsonism ```

Answer 30

Plant alkaloid obtained from Pilocarpus microphyllus Particularly active on the sweat and salivary glands and eyes; used as TX for xerostomia caused by Sjögren's syndrome or salivary gland dysfunction and for miosis induction, postop and following ophthalmic examination; second-line TX for chronic open-angle glaucoma

Answer 31

Muscarinic agonist In open-angle glaucoma, pilocarpine contracts the ciliary and circular muscles, producing miosis resulting in increased outflow of aqueous humor; in closed-angle glaucoma, pilocarpine-induced miosis opens the angle of the anterior chamber of the eye through which aqueous humor exits

Answer 32

0.5-6% ophthalmic solution has a duration of 4-14 hr; PO dose is usually 5-10 mg TID, has a 3-5 hr duration Ocusert® delivers pilocarpine for 7 days via a contact lens-like system

Answer 33

Blurred vision Exocrine glands: hypersalivation, diaphoresis Flushing Headache ``` Asthma Iritis Posterior synechiae (adhesion between iris and lens) Retinal detachment Heart disease Parkinsonism ```

Answer 34

Plant alkaloid obtained from Nicotiana tabacum | Used to help smokers quit smoking

Answer 35

Agonist at NM and NN receptors Complex action, affects CNS and all branches of peripheral nervous system; stimulates catecholamine release from adrenal medulla

Answer 36

Dosage forms: gum, lozenge, inhaler, nasal spray, transdermal patch Widely distributed in body tissues, especially CNS Mostly metabolized in liver; unchanged nicotine and metabolites are excreted by the kidney t1/2 = 30-120 min

Answer 37

CNS: dizziness, insomnia, irritability CV: ↑ BP and can have positive inotropic and chronotropic actions GI: constipation, diarrhea Angina, arrhythmia, myocardial infarction Caution in patients with hypertension, pheochromocytoma, insulin-dependent diabetes, vasospastic diseases, or thyroid disease resulting in thyrotoxicosis Pregnancy Risk Category D (transdermal)

Answer 38

Fast onset (

Answer 39

related to agonist activity at other AchR's: stim autonomic ganglia AchR (HTN, tachycard), and stim cardiac muscarinic R's (bradycard). Histamine release. Myalgias, incr intracranial and intraocular pressure, hyperkalemia (prolif of extrajunctional nAChRs, denervation, burns, trauma, prolonged immobility, myopathies)

Answer 40

Smoking cessation aid

Answer 41

High-affinity partial agonist a4b2 nicotinic receptors. Moderate affinity at 5-HT3 receptor.

Answer 42

0.5 and 1 mg tablets for PO use, 1 mg BID after one-week ramp up. Peak plasma conc after 3-4 hours, t1/2= 24 hours. Minimal metabolism, 92% excreted as is.

Answer 43

GI-related: transient nausea, constipation, flatulence. CNS: insomnia and vivid dreams Renal insufficiency (don't exceed 0.5 mg if in kidney failure). Risk of neuropsychiatric symptoms: hostility, irritability, agitation, depression, suicidal thoughts, attempted suicide.