Drugs for Midterm 3

Question 1

Disulfiram

Answer 1

Used to manage alcohol addiction
Can take it every day, no effects without alcohol
Causes extreme discomfort when alcohol is consumed
Flushing, headache, nausea, vomiting, sweating, hypotension and confusion
Binds to an inactivates aldehyde dehydrogenase

Question 2

Naltrexone

Answer 2

Will get abstinence in every 1 out of 10 people that you treat and significant reduction in everyone else
Functions as a competitive antagonist at opioid receptors and exhibits the highest affinity for the mu receptor isoform

Question 3

Acamprosate

Answer 3

Alters the activity of NMDA receptors
Highly dose dependent
Can lessen withdrawal and cravings

Question 4

Gabapentin and alcohol

Answer 4

Normalizes the stress-induced GABA activation in the amygdala that is associated with alcohol dependence

Question 5

2 inhibitors of ADH

Answer 5

Fomepizole
Ethanol
Can be used to treat ethylene glycol poisoning

Question 6

Buprenorphine

Answer 6

Partial agonist at opioid receptor with high affinity
Another way to treat opioid addiction (morphine)
It competes at the same site, but still gives some efficacy
Prevents the high, but also alleviates craving and drug seeking behaviour

Question 7

Prednisone

Answer 7

Decreases inflammation
Increases apoptosis of lymphocytes
Used to treat autoimmune diseases
Side effects: fluid retension, weight gain, increased blood sugar, osteopenia, hyperactivity

Question 8

Dexamethasone

Answer 8

Potent synthetic glucocorticoid class of steroid drugs
Anti inflammatory and immunosuppressant
More potent than prednisone

Question 9

How does
1. Alefacept
2. Etanercept
work to treat psoriasis?

Answer 9

1. Interferes with lymphocyte activation

2. Binds to TNFa and b and blocks binding with receptor

Question 10

Muromonab (OKT3)

Answer 10

Blocks killing by cytotoxic human T cells

Along with steroids, proved to be more effective at reversing acute rejection than did conventional steroid treatment

Question 11

Antithymocyte globulin

Answer 11

Antiserum from immunization of sheep/horses with human lymphoid cells
Antilymphocytes act on the small peripheral lymphocytes
With continued administration, thymus dependent lymphocytes are also depleted

Question 12

Basiliximab

Answer 12

Binds to the IL2 receptor on activated lymphocytes
Acts as an IL2 antagonist
Blocks IL2 from binding to activated lymphocytes
Same as Daclizumab
Organ transplants

Question 13

What would you use to treat MS exacerbations?

Answer 13

Synthetic adrenal glucocorticoids like prednisone
Want to dampen down the immune system and reduce IL 2
Inhibit the expression of pro-inflammatory genes

Question 14

Interferon-Beta

Answer 14

Slows the advance of the affliction and reduces the frequency of attacks
Subcutaneous injection
Reduces inflammation, maybe by promoting apoptosis of autoreactive immune cells
Side effects: flu like symptoms
For MS

Question 15

Glatiramer acetate

Answer 15

Random polymer composed of 4 amino acids that are found in myelin basic protein and may work as a decoy
Shifts the population of T cells from pro-inflammatory TH1 to regulatory TH2
Doesn’t extend the time between relapses
For MS

Question 16

Mitoxantrone

Answer 16

Type 2 topoisomerase inhibitor
Disrupts DNA synthesis and DNA repair in healthy and cancer cells
Suppresses the proliferation of T cells, B cells, and macrophages
Impairs antigen presentation and decreases pro inflammatory cytokines
For MS

Question 17

Tysabryi (Natalizumab)

Answer 17

Monoclonal antibody against alpha4 integrin
Interferes with the ability of immune cells to attach to endothelial cells and cross the BBB
For MS

Question 18

Fampridine-SP

Answer 18

Selective neuronal K+ channel blocker
By closing the exposed K channels in damaged fibers, the axon can transmit nerve impulses again
Improves walking and coordination
Does not alter disease progression
For MS

Question 19

Fingolimod

Answer 19

Sphingosine 1-phosphate receptor modulator
Sequesters lymphocytes in lymph nodes, preventing them from contributing to an autoimmune reaction
For MS

Question 20

Dimethyl Fumarate

Answer 20

Activates Nrf-2 increasing the expression of mitochondrial and anti-oxidant genes that reduce inflammation and protect oligodendrocytes and neuron
For MS

Question 21

Salbutamol

Answer 21

Beta 2 adrenergic receptor selective agent
Administered via inhalers
Bronchodilation achieved in 30 mins and effects last for 3-4 hours

Question 22

Caffeine, theophylline, theobromine

Answer 22

Methylxanthine drugs
2 actions:
1. Inhibits actions of PDE to increase stability of cAMP
2. Inhibits actions of adenosine by blocking adenosine receptors (block bronchoconstriction)
For asthma

Question 23

Atropine and ipratropium bromide

Answer 23

Antimuscarinic drugs
Block the effects of ACh at muscarinic receptors –> bronchodilation
Slightly less effective compared to beta agonists
For asthma

Question 24

Prednisone for asthma

Answer 24

Corticosteroids
Block production of cytokines by mast cells and eosinophils
Inhibit inflammation of asthmatic airways
Aerosol treatment is best
Can be used for prolonged periods safely

Question 25

Zileuton

Answer 25

5-lipoxygenase inhibitors
Inhibit the synthesis of leukotrienes by inhibiting the 5-lipoxygenase
For asthma

Question 26

Montelukast

Answer 26

Leukotriene receptor blocker
Inhibit the binding of leukotrienes to receptors in the target tissue
Administered orally
Very effective in reducing the frequency of bronchial exacerbations
Good for treating aspirin induced asthma

Question 27

Omalizumab

Answer 27

Anti-IgE monoclonal antibody

Block the actions of IgE in asthma

Question 28

Nifedipine and verapamil

Answer 28

Calcium channel blockers
Induce smooth muscle cell relaxation
Not as effective as salbutamol
For asthma

Question 29

Maraviroc (Celsentry)

Answer 29

Selective for CCR5
Blocks the CCR5-gp120 interaction (binds to CCR5)
Prevents CCR5 tropic HIV entry into cells

Question 30

Enfuvirtide (Fuzeon)

Answer 30

Mimics amino acids of HIV gp41 that are critical for viral/CD4 cell membrane fusion
Prevents viral entry
Attaches to gp41 and prevents the interaction

Question 31

Nucleoside reverse transcriptase inhibitors

Answer 31

Competitive inhibitors of reverse transcriptase
Compete with natural nucleosides
Inhibit chain elongation (lack the OH needed for bonding)

Question 32

Non-nucleoside reverse transcriptase inhibitors

Answer 32

Prevent HIV from using reverse transcriptase by binding at an allosteric site

Question 33

Protease inhibitors

Answer 33

Protease inhibitors prevent post-translational cleavage of Gag-Pol polyprotein
Results in immature, noninfectious viral particles
Prevents other cells from being infected

Question 34

Integrase inhibitors

Answer 34

Ex: Raltegravir
Binds viral integrase, inhibits strand transfer
Interferes with integration of reverse-transcribed HIV DNA (cDNA) into the chromosome of host cells

Question 35

Acyclovir

Answer 35

Used to treat herpes
Competition with deoxyGTP for the viral DNA polymerase resulting in:
1. it binding to the DNA template as an irreversible complex
2. chain termination following incorporation into the viral DNA

Question 36

Amantadine

Answer 36

For influenza

Blocks the M2 proton ion channel of the virus and inhibits uncoating of the viral mRNA

Question 37

Tamiflu (oseltamivir)

Answer 37

For influenza
Analog of sialic acid (decoy basically)
Interferes with the release of progeny influenza virus from infected to new host cells
Halts the spread of infection
Competitively and reversibly interacts with the active enzyme site to inhibit neuraminidase activity and destroy the receptors recognized by viruses