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Drug Mechs Final Conceptual
Terms in this set (47)
local anesthetics share what similar structures?
aromatic group on left
ester or amide group in middle
amine group on right
How do local anesthetics work?
•Stop propagation of action potentials in axon fibers
•Block voltage-gated Na+ channels (Nav)
-Physically plug pore
-Allosteric interaction with the channel
•Many show "Use-dependent block"
-Bind better to open channels or inactivated channels
(raises AP threshold)
what is the order of sensitivity for nerves to be blocked?
(most sensitive) Small myelinated -> non-myelinated -> large myelinated (least sensitive)
end result: motor fibers are less affected than sensory fibers
what are the unwanted affects of local anesthetics?
spread from local site to systemic circulation (by accident)
can cause confusion, agitation, convulsions or respiratory depression (could also mess with heart)
what is the third most common prescription drug taken by everyone?
what are the two distinct types of depression?
-~75% "reactive depression"
•Stress related, not genetic
-~25% "endogenous depression"
•Familial pattern, but no identified genes
-Less common than unipolar, hereditary
-Oscillates between manic and depressive
what areas of the brain are responsible for depression?
What is the monoamine theory of depression?
•(1965) Depression is a result of low monoamine transmitters
-Norepinephrine & 5-HT
•Reuptake blockers as pharmacological agents
-Block occurs within minutes
-Antidepressant effects do not appear for several weeks, regardless of class
•Block of either appears to work, some people respond better to one than the other
what are other possible explanations for depression?
altered glutamate transmission (depression has higher levels)
Selectivity of reuptake inhibition
what percent of patients fail to improve with antidepressants?
(better for moderate to severe)
what are the possible side effects of ssri's
•nausea, anorexia, insomnia, loss of libido
what are the side effects of TCA's?
•initial use -> sedation, confusion, motor impairment (these effects tend to wear off after a few days). Other effects: dry mouth, blurred vision, urinary retention, postural hypotension, continued sedation in some, overdose -> ventricular dysrhythmias
what are the side effects of Monoamine receptor antagonists?
constipation, increased appetite, weight gain, somnolence
what are the side effects of MAOI's
•hypotension, tremors, excitement, insomnia, increased appetite, weight gain, dry mouth, blurred vision, urinary retention, and in rare cases hepatotoxicity. Also have interactions with foods (containing tyramine, i.e., cheese and fermented compounds) and other drugs, i.e., OTC ephedrine -> severe hypertension
-Drug interactions can be life-threatening
what are other clinical uses for antidepressants?
•TCAs for neuropathic pain
•TCAs and SSRIs for fibromyalgia
•SSRIs for anxiety disorders
•SSRIs for ADHD
•Buproprion (NE uptake blocker) for addiction
what are other more non-traditional depression treatments?
electroconvulsive therapy (shock the brain)
effective in 60-80%
can cause confusion and memory loss
transcranial magnetic stimulation
uses magnetic field instead of electricity
how does bipolar depression need to be treated differently?
normal antidepressants can induce a "manic phase" so they use mood stabilizing drugs like Lithium
what are the main drugs of abuse?
what drugs of abuse score highest on harm to self and others?
drugs can induce dependence (2 types)
•After experiencing a "rewarding" effect à desire to repeat
•Can give rise to intense cravings
•Can be triggered by environmental cues
-Places, people, paraphernalia
•May also include desire to avoid withdrawal symptoms
•Characterized by withdrawal syndrome upon cessation of the drug or administration of an antagonist
•Adverse physiological effects
-Could last over days or weeks
-Depends on the drug involved
what parts of the brain are involved in dependence?
•The "mesolimbic dopaminergic pathway"
-Ventral tegmental area (VTA)
•Dopamine is one of the major neurotransmitters in this pathway
vaccine for some drugs to bind and prevent them from crossing the blood brain barrier
who first observed penicillin?
Andrew Flemming in 1928
purple (simple cell wall)
pink (more advanced cell wall)
can be more resistant to antibiotics
What are sulfonamides?
•Discovered in the 1930s
•Bacteriostatic not bactericidal
•Not used as much any more because of increasing bacterial resistance
What are B-lactam antibiotics?
•Penicillin was the first (now have many)
•Was extremely effective bactericidal agent
•Resistance occurs with b-lactamase enzymes
-Can be passed between bacteria
•Interferes with bacterial cell wall synthesis à bacterial cell lysis
•Can be given by mouth or i.v.
•Relatively little toxicity
what are protein synthesis inhibitors?
-Broad spectrum, given orally, bacteriostatic
-Resistance can be passed between bacteria by plasmid
-Side Effects: Chelate Ca++ - > can be deposited in growing teeth and bones -> discolorations
-Can also induce phototoxicity -> rash from sunlight
stuff to know about viruses
•Small infective agents
•Can be either RNA or DNA
•Can be either single or double stranded
Rely on host cell's machinery to reproduce
Can't reproduce on their own
DNA viruses usually enter the nucleus to reproduce
RNA viruses usually reproduce in the cytoplasm
RNA retroviruses: RNAàDNAàRNA
*Requires viral reverse transcriptase enzyme
how do killer t cells function?
MHC-1 expression alteration (CD8+ killer T cell)
how do anti viral drugs work?
•Commonly inhibit DNA or RNA synthesis
•Usually attack specific mechanisms used by the virus to replicate and infect cells
•Specificity limits side effects
•Drugs tend to be specific for a particular virus
•Many end in -vir (but not all)
what is HAAT
Highly Active Antiviral Therapy
A 3 or 4 drug combination for HIV treatment
what are interferons?
•Family of hormones that regulate immune function
•Induce the production of enzymes in host cell that inhibit viral translation
•At least 3 types: a, b, g
what is a pooled immunoglobulin?
•Antibodies pooled from donated blood
•Can be used prophylactically to prevent or attenuate several types of viral infections
what is considered a tumor?
•an abnormal new growth of tissue that possesses no physiological function and arises from uncontrolled, usually rapid cellular proliferation
what is a neoplasm?
what happens for a cell to become cancerous?
-Conversion of proto oncogenes -> oncogenes
•About 100 oncogenes have been identified
-Inactivation of tumor suppressor genes
•About 30 tumor suppressor genes have been identified
what are the different types of cells in a tumor?
-Group A: continuously dividing cells
•The most susceptible group of cells to current chemotherapy, but may make up as little as 5% of overall tumor cells
-Group B: G0 phase cells
•Not currently dividing, but capable of doing so
-Group C: cells incapable of cell division
what classes of chemotheraputic drugs are there?
alkylating and related agents
protein kinase inhibitors
what types of resistance can occur to anticancer drugs
primary (resistant first time drug is given)
aquired (tumor is suceptable at first but then becomes resistant via adaptation, mutation)
how many total proteins in body?
how many proteins are "druggable"?
what are the 4 stages of preclinical development?
1: Safety pharmacology: no immediate adverse effects from administration of compound
2: Preliminary toxicology testing: i.e., toxicities from extended dosing (daily for 28 days, in at least 2 different species), with autopsies etc.
3: Pharmacokinetic testing (ADME)
4: Chemical and pharmaceutical testing: large scale synthesis feasibility, compound stability, etc.
What are the stages of clinical development?1
Phase I clinical trials: small group (20-80) of healthy volunteers
Identify any potentially dangerous effects in humans
Tolerability: identify any unwanted effects (headache, nausea, drowsiness, etc.)
Pharmacokinetics: ADME in humans
Phase II clinical trials: little bit larger group (100-300) of affected patients
Test for efficacy
Establish effective doses
May include several populations to examine more than one condition (i.e., depression, anxiety, phobias, etc.) to see if compound works for different things
Phase III clinical trials: larger group (1000s) of affected patients
Gold standard is the double-blind, randomized trial
Compare safety and efficacy of new treatment versus standard treatments
Very costly to run, difficult to organize, and generally take many years to complete
"Phase IV" studies: continual monitoring of drug after approval for potentially serious side-effects not previously identified
May need to limit the use of a drug to a particular subpopulation
May need to pull a drug off the market
other clinical trial stuff
1 in 50 projects is a sucessful drug
4 billion$ cost
patent filed at end of discovery phase
1/3 of drugs turn a profit for a company
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