Drugs for Midterm 3 Flashcards
Disulfiram
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
Naltrexone
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
Acamprosate
Alters the activity of NMDA receptors
Highly dose dependent
Can lessen withdrawal and cravings
Gabapentin and alcohol
Normalizes the stress-induced GABA activation in the amygdala that is associated with alcohol dependence
2 inhibitors of ADH
Fomepizole
Ethanol
Can be used to treat ethylene glycol poisoning
Buprenorphine
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
Prednisone
Decreases inflammation
Increases apoptosis of lymphocytes
Used to treat autoimmune diseases
Side effects: fluid retension, weight gain, increased blood sugar, osteopenia, hyperactivity
Dexamethasone
Potent synthetic glucocorticoid class of steroid drugs
Anti inflammatory and immunosuppressant
More potent than prednisone
How does
1. Alefacept
2. Etanercept
work to treat psoriasis?
- Interferes with lymphocyte activation
2. Binds to TNFa and b and blocks binding with receptor
Muromonab (OKT3)
Blocks killing by cytotoxic human T cells
Along with steroids, proved to be more effective at reversing acute rejection than did conventional steroid treatment
Antithymocyte globulin
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
Basiliximab
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
What would you use to treat MS exacerbations?
Synthetic adrenal glucocorticoids like prednisone
Want to dampen down the immune system and reduce IL 2
Inhibit the expression of pro-inflammatory genes
Interferon-Beta
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
Glatiramer acetate
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
Mitoxantrone
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
Tysabryi (Natalizumab)
Monoclonal antibody against alpha4 integrin
Interferes with the ability of immune cells to attach to endothelial cells and cross the BBB
For MS
Fampridine-SP
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
Fingolimod
Sphingosine 1-phosphate receptor modulator
Sequesters lymphocytes in lymph nodes, preventing them from contributing to an autoimmune reaction
For MS
Dimethyl Fumarate
Activates Nrf-2 increasing the expression of mitochondrial and anti-oxidant genes that reduce inflammation and protect oligodendrocytes and neuron
For MS
Salbutamol
Beta 2 adrenergic receptor selective agent
Administered via inhalers
Bronchodilation achieved in 30 mins and effects last for 3-4 hours
Caffeine, theophylline, theobromine
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
Atropine and ipratropium bromide
Antimuscarinic drugs
Block the effects of ACh at muscarinic receptors –> bronchodilation
Slightly less effective compared to beta agonists
For asthma
Prednisone for asthma
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
Zileuton
5-lipoxygenase inhibitors
Inhibit the synthesis of leukotrienes by inhibiting the 5-lipoxygenase
For asthma
Montelukast
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
Omalizumab
Anti-IgE monoclonal antibody
Block the actions of IgE in asthma
Nifedipine and verapamil
Calcium channel blockers
Induce smooth muscle cell relaxation
Not as effective as salbutamol
For asthma
Maraviroc (Celsentry)
Selective for CCR5
Blocks the CCR5-gp120 interaction (binds to CCR5)
Prevents CCR5 tropic HIV entry into cells
Enfuvirtide (Fuzeon)
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
Nucleoside reverse transcriptase inhibitors
Competitive inhibitors of reverse transcriptase
Compete with natural nucleosides
Inhibit chain elongation (lack the OH needed for bonding)
Non-nucleoside reverse transcriptase inhibitors
Prevent HIV from using reverse transcriptase by binding at an allosteric site
Protease inhibitors
Protease inhibitors prevent post-translational cleavage of Gag-Pol polyprotein
Results in immature, noninfectious viral particles
Prevents other cells from being infected
Integrase inhibitors
Ex: Raltegravir
Binds viral integrase, inhibits strand transfer
Interferes with integration of reverse-transcribed HIV DNA (cDNA) into the chromosome of host cells
Acyclovir
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
Amantadine
For influenza
Blocks the M2 proton ion channel of the virus and inhibits uncoating of the viral mRNA
Tamiflu (oseltamivir)
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
