Term
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Definition
Dr. Fay
fam, fa, fur, fox, tea |
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Term
| IMIPRAMINE (Tofranil, Janimine) |
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Definition
tricyclic antidepressant (the prototype)
The antidepressant FX take 2-4 weeks. Also used to treat OCD, panic attacks, generalized anxiety, social phobias, also in child bed-wetting. MofA not well understood but probably b/c it inhibits synaptic reuptake of NE and S. Experience sedation (counter-intuitive), but also CNS stimulation (which explains tremors, decreased seizure threshhold, and possibly provoking manias in bipolar pt's)
Side FX include anticholinergic (dry mouth, constipation, etc.); cardiovascular FX (postural hypotension, tachycardia, arryhtmias) CNS FX (tremor, Parkinsonism, etc.); weight gain; male sexual dysfunction; possible teratogen; rare but fatal blood dyscrasias |
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Term
| What's the advantage of the second generation antidepressants (e.g. SSRIs) over the older drugs used to treat depression (e.g. tricyclic antidepressants)? |
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Definition
Fewer cardiovascular side FX
& a lot less likely to wind up in fatal overdose
(these drugs are not more effective, just safer to use) |
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Term
| What happens to the neurons in the body as antidepressant medications are taken chronically over a long-term period? |
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Definition
Initially, antidepressants function to inhibit the synaptic reuptake of neurotransmitter amines (NE, 5-HT, or DA … see the chart on p. 13)
Over time, the density and sensitivity of the receptors for those neurotransmitter amines begins to change (e.g. beta receptors decrease in density) |
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Term
| T/F: Antidepressant medications have a broad therapeutic window, with wide ranges of effective dosage regimens |
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Definition
FALSE
Antidepressants have narrow therapeutic windows, so be aware of the side FX |
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Term
| What does acute poisoning from antidepressant medications look like? How would you treat it? |
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Definition
CNS agitation, the classic anticholinergic symptoms, tachycardia, hypotension, arrythmias, seizures (in the extreme case)
Tx with gastric charcoal to absorb the drug; sodium bicarbonate to buffer against acidosis and cardiovascular comlications. Lidocaine and Physostigmine do not help. Also, beware that these pt's may be suicidal, so don't px them any meds beyond a lethal dose. |
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Term
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Definition
| When pt is on tricyclic antidepressants and MAO inhibitors, they can get excessively high levels of synaptic serotonin. This severe drug intxn is characterized by tremors, hypertension, high fever, and seizures. Extremely hard to treat, which is why it's recommended to wait 2-4 weeks after stopping a tricyclic Rx before taking a MAO inhibitor. |
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Term
| What drugs besides antidepressants are also prescribed for depression? |
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Definition
Benzos (Xanax), Anxiolytics (Valium)
not stimulants |
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Term
| How do MAO inhibitors work? How often are they prescribed? |
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Definition
MAO inhibitors stop the enzyme (MAO) responsible for breaking down neurotransmitter amines
They are considered very much backup drugs (to SSRIs) in the treatment of depression, because they come with drug-drug and drug-food interactions. And non-specific MAO-A/MAO-B inhibitors have even more side FX. |
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Term
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Definition
Tricyclic Antidepressant
Same as Imipramine,
except more sedating and more anticholinergic activity |
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Term
What does SSRI stand for?
What does SNRI stand for? |
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Definition
SSRI = Selective Serotonin Reuptake Inhibitor
SNRI = Serotonin-Norepinephrine Reuptake Inhibitor |
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Term
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Definition
SSRI Antidepressant (the prototype)
No more effective than Imipramine, but better side FX profile. Fluoxetine used to treat depression, OCD, anxiety, and premenstrual dysphoric disorder. MofA is not well understood but likely due to inhibition of synaptic reuptake of Serotonin (@5-HT).
Much less sedating, less anticholinergic, and less cardiovascular complications with Fluoxetine; but can cause headache, anxiety, tremor, agitation, nausea, and sexual dysfunction in males. Fluoxetine metabolized in the liver, so potential for many drug-drug intxns. |
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Term
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Definition
SSRI Antidepressant
Similar to Fluoxetine, except longer-acting (T1/2 = 24hrs … protects against discontinuation problems) and Sertraline is much less likely for CYP drug intxns in the liver. |
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Term
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Definition
SSRI Antidepressant
Like Fluoxetine, but shorter-acting (T1/2 = 10hrs).
Paroxetine produces more weight gain than other SSRIs, and also has more drug-drug intxns |
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Term
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Definition
SSRI Antidepressant
One of the newest SSRIs (approved in 1998). Similar to Sertraline (longer-acting and fewer drug-drug intxns) |
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Term
|
Definition
SSRI Antidepressant
One of the newest SSRIs (approved in 1998). Similar to Sertraline (longer-acting and fewer drug-drug intxns) |
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Term
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Definition
SNRI Antidepressant
Inhibits synaptic reuptake of NE, S and DA. Used for tx of depression and generalized anxiety. May have a mild stimulant effect (possible use for ADHD), and would be good choice for pt's refractory to SSRIs.
Venlafaxine seems to have fewer cardiovascular complications than the SSRIs, although it does sometimes cause hypertension and tachycardia; other side FX are nause, nervousness, anxiety, seating, sexual dysfunction. More drug-drug intxns (due to both NE/5-HT inhibition) |
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Term
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Definition
SNRI Antidepressant
Inhibits synaptic reuptake of NE, S and DA. Used for tx of depression and generalized anxiety. May have a mild stimulant effect (possible use for ADHD), and would be good choice for pt's refractory to SSRIs.
Venlafaxine seems to have fewer cardiovascular complications than the SSRIs, although it does sometimes cause hypertension and tachycardia; other side FX are nause, nervousness, anxiety, seating, sexual dysfunction. More drug-drug intxns (due to both NE/5-HT inhibition) |
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Term
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Definition
SNRI Antidepressant
Newer drug that resembles Venlafaxine (SNRI backup to SSRI, fewer CV effects, but more drug-drug intxns). Also approved as a pain reliever for musculoskeletal and neuropathic pain. |
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Term
|
Definition
Antidepressant (2nd generation)
Blocks 5-HT2 receptors and inhibits Serotonin reuptake. Trazodone is very sedating, and some pt's will use as nighttime Rx before bed.
Fewer anticholinergic and cardiovascular FX, but very sedating (above), and also associated with priapism (a permanent erection that can lead to impotence) |
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Term
|
Definition
Antidepressant (2nd Generation)
Similar to Trazodone (fewer anticholinergic FX, fewer cardiovascular complications, but very sedating) |
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Term
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Definition
Antidepressant (2nd generation)
Unique antidepressant that selectively inhibits DA reuptake. Used for addiction (to nicotine, cocaine, etc.), and exhibits a mild stimulant effect ("psychic energizer").
More likely to cause seizures/tremor (b/c dopaminergic action), but less likely to have sexual problems |
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Term
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Definition
Antidepressant (NE-selective)
Atomoxetine is a selective norepinephrine reuptake inhibitor that is approved for the treatment of ADHD in children and adults (even though it's not a stimulant).
Side FX include suppression of appetite, decreased weight gain, increased blood pressure, tachycardia, sexual dysfunction in males. |
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Term
| What is the difference between MAO-A and MAO-B enzymes? |
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Definition
MAO-A preferentially metabolizes NE and 5-HT, so MAO-A inhibitors are commonly used as antidepressants
MAO-B preferentially metabolizes DA, so MAO-B inhibitors are used alone or in combination to treat Alzheimer's and Parkinson's Disease |
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Term
|
Definition
MAO Inhibitor Antidepressant
MAO-A inhibitor (increase NE and 5-HT) used as a third-line backup antidepressant (slow onset, takes several weeks), to treat bulimia, to treat OCD, and can have stimulatory effect (treat narcolepsy). Long-acting drug that binds irreversibly to MAO-A
Side FX include orthostatic hypotension, hypertension (in overdose), GI FX, nausea, vertigo, CNS stimulation, liver damage, allergic reactions. The single greatest problem associated with MAO inhibitors though is lethal drug-food interactions (tyramine-containing, "cheese toxicity") |
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Term
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Definition
| MAO inhibitors can be involved in a potentially lethal interaction with foods containing tyramine, such as cheese, bananas, avocado, soy, wine, beer, meats - that can cause severe hypertension, fever, and convulsions. Potentiation of sympathomimetic agents |
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Term
| TRANYLCYPROMINE (Parnate) |
|
Definition
MAO Inhibitor Antidepressant
Similar to Phenylzine (long-acting MAO-A inhibitor, backup antidepressant, possible cheese toxicity w/ tyramine foods) |
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Term
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Definition
MAO-B Inhibitor Antidepressant
Selegiline is a selective MAO-B inhibitor used for the treatment of Parkinson's Disease, also as a transdermal patch for depression. Slow onset, takes several weeks, can have some stimulatory FX.
Adverse FX are hypotension, hypertension (in overdose), but less potential for peripheral side FX associated with MAO-A inhibitors. Selegiline does not undergo classic interactions with tyramine (cheese toxicity) at recommended doses. |
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Term
| LITHIUM CARBONATE (Eskalith) |
|
Definition
Simple Salt for Bipolar Disorder
Lithium works really well (~80%), but it's really dangerous and requires the pt to get bloodwork done monthly to monitor absorption (b/c it's therapeutic index is really low). T1/2 = 24hrs, so you have to wait a couple days to reach steady-state. The MofA for lithium is not well understood - it's not a stimulant and not a depressant, but it reduces fluctuations in mood.
The major adverse FX have to do with renal toxicity. Lithium toxicity is compounded by sodium Na+ depletion, so concurrent use of Lithium with diuretics (e.g. thiazides) is hazardous. Also, any drugs altering renal function (incl. NSAIDs) will also alter lithium excretion. Many serious drug intxns are possible with Lithium |
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Term
| What does Lithium toxicity look like? How do you treat? |
|
Definition
GI nausea/vomiting, CNS FX, slurred speech, dizziness, confusion, hypotension, arrythmias, shock (in severe cases)
Tx by removing the drug, maintaining fluids and electrolytes, administer anticonvulsants and/or antiarrythmics as needed, induce diuresis (osmotic mannitol), hemodialysis |
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Term
|
Definition
Anticonvulsant Drug for Mania
May now becoming front-line drug for treatment of manic depressives and/or bipolar disorders |
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Term
| VALPROIC ACID ANALOGS (Depakene, Depakote) |
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Definition
Anticonvulsant Drug for Mania
May now becoming front-line drug for treatment of manic depressives and/or bipolar disorders, also used for migraines |
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Term
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Definition
Anticonvulsant Drug for Mania
A chloro-nitrobenzodiazepine, this anticonvulsant and muscle relaxant may now becoming front-line drug for treatment of manic depressives and/or bipolar disorders |
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Term
| What other drugs besides Lithium can be used for bipolar disorder? |
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Definition
Benzodiazepines
Antipsychotics
Gabapentin |
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Term
| AMPHETAMINE (Benzedrine, Biphetamine, Adderall) |
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Definition
CNS STIMULANT (the prototype)
Amphetamine stimulates arousal and wakefulness and focus, especially on boring repetitive tasks. Used for narcolepsy and "hyperkinetic syndrome" (ADHD) in children, also weight reduction for obesity. Delayed fatigue, suppression of appetite, tolerance and dependence may develop.
The dopaminergic suppression of Amphetamines may lead to Parkinson's ("High Hitler"). Produces euphoria "high", which can end in rebound "crashing", leading to cycles of abuse. Can cause "tactile hallucinations" of itching, hypertension, tachycardia, arrythmias, widely dilated pupils. Amphetamine can lead to emotional lability/volatility; the suppression of appetite can lead to malnutrition; and "meth mouth" is a nasty dental problem |
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Term
| d-AMPHETAMINE (Dexedrine, Biphetamine, Adderall) |
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Definition
CNS Stimulant
Same as Amphetamine |
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Term
| LISDEXAMFETAMINE (Vyvanse) |
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Definition
CNS Stimulant
Similar to Amphetamine
Lisdexamfetamine is a prodrug with long-acting formulations that may help kids who take Rx at school |
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Term
METHAMPHETAMINE (Desoxyn)
"speed" |
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Definition
CNS Stimulant (The prototype)
Similar to Amphetamine
Methamphetamine produces very intense CNS FX and is very widely abused (the smokeable form similar to "crack" is much longer-acting, 12hrs)
Chronic abusers may experience dental problems ("meth mouth") or lung damage from smoking |
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Term
| METHYLPHENIDATE (Ritalin) |
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Definition
CNS Stimulant
Shorter-acting than Amphetamines, but otherwise similar pharmacologically. Used to treat ADHD in kids |
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Term
| How do the amphetamines work in the brain/body? |
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Definition
| Enhance the release and inhibit the uptake of NE and DA (acute effect) with possible direct stimulation of alpha receptors in the "reward centers" of the brain (i.e. locus ceruleus) |
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Term
|
Definition
CNS Stimulant
Similar to Amphetamines. Found in leaves in Eastern Africa and Middle East. Relatively easy to synthesize and was marketed recently as "bath salts" in the US. Banned by the DEA |
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Term
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Definition
CNS Stimulant
Used medically as a sympathomimetic, also in OTC "pep pills", though the FDA has banned ephedrine for supplements (several athletes died).
Ephedrine is not the same as Pseudoephedrine (used as a nasal decongestant) |
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Term
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Definition
CNS Stimulant
Newer drug used for narcolepsy and "shift work disorders". MofA is not clear but may cause DA increase (reinforcing action). Modafanil is not technically an amphetamine, but it has many amphetamine-like FX on wakefulness. |
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Term
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Definition
CNS Stimulant
Newer drug used for narcolepsy and "shift work disorders". MofA is not clear but may cause DA increase (reinforcing action). Armodafanil is not technically an amphetamine, but it has many amphetamine-like FX on wakefulness. |
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Term
|
Definition
CNS Stimulant
Cocaine's uses and effects are identical to the amphetamines (stimulant, euphoria, increased confidence, suppression of appetite, reinforcing behavior). Also used as a local anesthetic since 1800s. The MofA involves inhibition of synaptic reuptake of DA, increasing synaptic DA levels (although in chronic use the neurons start producing less DA). Tolerance and dependence develop readily
White powder = Cocaine-HCl (water-soluble salt)
"Crack" = Cocaine (treated to elute out -HCl, not water-soluble so it's smoked)
Can get hypertension, tachycardia, arrhythmias leading to sudden death, mydriasis, teratogenic effects on the fetus, risk of nasal damage with snorting, risk of lung damage with smoking, risk of infection with IV use |
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Term
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Definition
| most commonly seen in drug abusers taking high doses, although sometimes at therapeutic doses, amphetamine and cocaine (ab)users may exhibit symptoms of organic psychosis including hallucinations, thought disorder, aggression, dilated pupils, arrythmia, hypertension, hyperthermia, rapid breathing, restlessness, seizures, tremor, catatonia or stupor |
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Term
| How would you treat addictive disorders (for cocaine, etc.)? |
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Definition
The acute FX of stimulant use can be inhibited sometimes by antipsychotics
Tx addictive disorders w/ nutritional supplements, l-DOPA, bupropion |
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Term
|
Definition
CNS Stimulant
Everyday use as a stimulant beverage; medical use for asthma and for pain relief with headaches and as a diuretic. Caffeine is a CNS stimulant that is distinct from amphetamines and cocaine but with some overlapping FX. Does improve mental function and stimulate respiration; people do become tolerant and dependent. It's physically reinforcing and caffeine withdrawal syndrome can be serious. The MofA theory is that it inhibits adenosine receptors.
Health FX are relatively benign. Stimulates gastric acid (so avoid in pt's with peptic ulcers). Caffeine overdose is possible (with seizures), and can get excessive cardiac stimulation. |
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Term
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Definition
CNS Stimulant
Similar to caffeine
Theophylline relaxes bronchioles (at high doses) and is used for asthma |
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Term
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Definition
CNS Stimulant
Similar to caffeine
Aminophylline relaxes bronchioles (at high doses) and is used for severe asthma |
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Term
| What is the phsyiological function of thyroid hormone? What is necessary for its production? And how would abnormal levels of this hormone manifest in a patient? |
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Definition
| Thyroid hormone primarily controls the basal metabolic rate, so unexplained weight gain and/or weight loss are two key indicators of abnormal thyroid hormone levels or activity. The thyroid gland is one of the largest endocrine glands in adults. And a prerequisite of thyroid hormone production is iodide trapping (I2 and I-) |
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Term
| What is the difference between T4 and T3? |
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Definition
T3 is the active form
T4 is converted to T3 by a deiodinase enzyme at peripheral effector cells
The end result is neuronal excitation (which can be dangerous for cardiac arrythmias), increased lipolysis which depletes glycogen stores, increased cholesterol production and secretion
T3 and T4 act in a negative feedback loop back on the pituitary, suppressing TSH release |
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Term
| LEVOTHRYOXINE (Synthroid, Levoxyl) |
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Definition
Synthetic T4
Used to treat hypothyroidism, which may manifest as weight gain and lethargy or goiter, always low T3/T4. With Levothryoxine, synthetic T4 gets converted to T3, essentially replacement therapy |
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Term
|
Definition
congenital hypothyroidism
(1 in 3,500 births)
signs and sx of cretinism include lethargy, postnatal jaundice, protruding abdomen, thick tongue, severe mental retardation, stunted growth |
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Term
| What are the four major causes of adult hypothyroidism? |
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Definition
(1) Hasimoto thyroiditis => most common in the use, 4x more common in females, low T3/T4, but high TSH
(2) Simple colloid goiter => from chronic inadequate I- intake, low T3/T4 results in increased TSH, and increased thyroid gland growth (ironically)
(3) Idiopathic or nontoxic colloid goiter => adequate I- intake, but the goitrogens in the diet inhibit I- transport, low T3/T4
(4) Postpartum thyroiditis => happens in 8-10% of all women after pregnancy, antibodies damage thyroid tissue, producing first hyperthyroidism, then hypothyroidism |
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Term
| What are the signs and sx of hypERthyroidism? What is the most common cause? How do you treat? |
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Definition
Hyperthyroidism sx => weight loss, nervousness, restlessness, hot moist skin, heat intolerance, fatigue, weakness and muscle cramps. Can see normal T3/T4, but low TSH
Most common cause of hyperthyroidism is Graves disease (aka diffuse toxic goiter, aka autoimmune hyperthyroidism) and is 6x more common in women. IgG antibodies mimic TSH and increase T4/T3, suppressing TSH production to zero. Eventually, may become hypothyroid
Tx for hyperthyroidism is with iodides, which inhibit TSH synthesis |
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Term
|
Definition
Low bone mass
Greater probability of bone fracture
Type I => lack of estrogen post-menopause
Type II => inadequate Ca2+ intake and/or excessive PTH activity |
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Term
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Definition
Bisphosphonate
Used to treat osteoporosis, Paget's. MofA is by inhibiting enzymes in osteoclasts, slows down bone turnover, increases bone density, reduced fractures. Alendronate is more potent and longer-lasting than the other bisphosphonates
Side FX include GI distress, esophageal erosion |
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Term
|
Definition
Bisphosphonate
Used to treat osteoporosis, Paget's. Chemically different from the other bisphosphonates but achieves same results (reduced bone turnover, increased bone density, decreases in fractures)
Side FX include GI distress, esophageal erosion. You need to take a large glass of water and sit for 30min |
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Term
| ZOLEDRONATE (Zometa, Reclast) and ZOLEDRONIC ACID |
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Definition
Bisphosphonates
Administered IV once a year for the treatment of Osteoporosis and Paget's
Side FX of fever, nausea, constipation, diarrhea, vomiting, GI pain |
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Term
|
Definition
Bisphosphonate
Similar to other bisphosphonates (Alendronate, Risedronate) |
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Term
|
Definition
Estrogen Therapy
Selective Estrogen Receptor agonist in bone, formerly used for the treatment of postmenopausal osteoporosis in women
But risks outweighed benefits => venous thromboembolism, increased breast cancer, coronary heart disease |
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Term
|
Definition
Parathyroid Hormone replacement
Teriparatide is replacement PTH for treatment of postmenopausal osteoporosis. Appears to work better than Alendronate, but very expensive
Side FX of nausea, dizziness, leg cramps |
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Term
| CALCITROL (1,25-hydroxyvitamin-D) |
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Definition
Vitamin D
Calcitrol is a Vitamin D metabolite that increases Ca2+ absorption and decreases Ca2+ excretion. Used for osteoporosis and hypoparathyroidism, with decreased bone resorption, increased osteoblast recruitment, marked reduction in fractures.
Few side FX; does not depend on liver or kidneys for activation |
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Term
| What are the major causes of hypercalcemia? What are the signs and sx? |
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Definition
Primarily breast and lung cancer pt's where tumors release PTH, increasing bone resorption
Signs and Sx are weakness, lethargy, nausea, polyuria |
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Term
| Osteonecrosis of the jaw is a side effect for which class of drugs? |
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Definition
| Bisphosphonates (especially from multiple injections of Zoledronate) suppress osteoclast activity, which also prevents bone resorption and repair in ischemically-damaged cancellous bone (of the jaw) |
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Term
|
Definition
Bisphosphonate
Used to treat osteoporosis. But also used to treat hypercalcemia (of malignancy). Reduces bone pain and fractures in multiple myeloma and breast cancer pt's
Only available IV injection; drug is very expensive
Side FX include nausea, anorexia, leukopenia, pain at injection site. |
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Term
| What drugs are used to treat hypercalcemia? |
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Definition
Injectable IV bisphosphonates (Zoledronate & Pamidronate) inhibit osteoclast activity
Loop diuretics (Furosemide) increase Ca2+ secretion
Glucocorticoids inbhibit Ca2+ absorption
Calcitonin/Calcimar/Cibacalcin inhibit osteolysis and increase Ca2+ secretion |
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Term
|
Definition
a bone abnormality caused by overactive osteoclasts, leading to increased bone turnover and abnormal bone formation (misshapen)
Tx with calcitonin or a bisphosphonate (esp. long-acting Alendronate) to inhibit osteolysis and prevent abnormal bone formation |
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Term
| What are the signs and sx of hypoPARAthyroidism? How would you treat? |
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Definition
Signs and sx => hypocalcemia (not enough PTH), tetany (neuromuscular) and seizures (70%)
Tx with Vitamin D (Calcitriol) |
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Term
|
Definition
Antihelminth
One of the preferred drugs for infection by pinworm, roundworm, nemotode, hookworm
MofA is by inhibition of microtubule polymerization and microtubule-dependent glucose uptake in parasites, with little or no effect on mammalian cells.
Most common side FX with Mebendazole are GI-related, potential teratogen |
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Term
|
Definition
Antihelminth
One of the preferred drugs for infection by pinworm, roundworm, nemotode, hookworm
MofA is by inhibition of microtubule polymerization and microtubule-dependent glucose uptake in parasites, with little or no effect on mammalian cells.
Albendazole common side FX are GI-related, potential teratogen, causes hepatotoxicity, can cause leukopenia |
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Term
| PYRANTEL PAMOATE (Antiminth) |
|
Definition
Antihelminth
Broad spectrum agent effective against a variety of nematodes (including roundworm, pinworm, hookworm). Causes depolarizing muscular blockade, paralyzes parasites, which get expelled during peristalsis.
Side FX are not too severe, GI upset, use in caution with pre-existing liver failure |
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Term
| PRAZIQUANTEL (Biltricide) |
|
Definition
Antihelminth
Broad spectrum antihelminthic drug used against cestodes (tapeworm) and trematodes (schisto). MofA is altered Ca2+-influx, inducing muscle contraction and spastic paralysis, causes the worm's suckers to become dislodged from blood vessel and end up getting phagocytosed in the liver
Praziquantel has little effect on human muscle contraction. Side FX are mild, dizziness, headache, GI pain, nausea/vomiting, with increase in liver enzymes |
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Term
|
Definition
Antiprotozoal (non-malarial)
Metronidazole is a -cidal drug that inhibits DNA synthesis. Good activity against anaerobic bacteria (bacterioides fragilis, c. difficile), and against E. histolytica, Trichomonas vaginalis and preferred drug for treating Giardiasis (infectious diarrhea) from anal-oral contact or drinking contaminated water, which produces watery foul-smelling diarrhea
Drug intxns with alcohol, nausea, headache, dry mouth, carcinogenic (avoid in first trimester pregnancy) |
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Term
| IODOQUINOL (Yodoxin, Diquinol) |
|
Definition
Antiprotozoal (non-malarial)
Iodoquinol MofA is unknown, but it is effective against E. histolytica (used in combination with Metronidazole)
Toxicity, neurotoxicity can lead to optic neuritis and loss of vision |
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Term
| PAROMYCIN SULFATE (Humantin) |
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Definition
Antiprotozoal (non-malarial)
Aminoglycoside that inhibits protein synthesis via binding to the 30S ribosomal subunit. Has good activity against E. histolytica (used in combination with Metronidazole to treat amebiasis) and in AIDS patients, paromomycin is a drug of choice
Side FX are GI (anorexia, nausea, vomiting, diarrhea), potential for nephrotoxicity, ototoxicity, and neuromuscular blocking effects like other aminoglycosides |
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Term
| What kinds of pt's are at risk of protozoal infection? |
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Definition
| Opportunistic infections with protozoa are prominent in infants, individuals with cancer, transplant recipients, those receiving immunosuppressive drugs, and persons with AIDS |
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Term
| How do protozoal infections present clinically? |
|
Definition
E. histolytica => amebiasis => severe, bloody diarrhea
Giardia lamblia => Giardiasis => profuse watery foul-smelling diarrhea
Trichomonas vaginalis => trichomoniasis => sexually-transmitted, males are often asymptomatic carriers, symptomatic females may exhibit smelly yellow-green discharge, valvular pruritis, dysuria and a strawberry vagina |
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Term
| For what infections do you use Mebendazole/Albendazole? And which do you use Praziquantel? |
|
Definition
Pinworm => Me/Al
Roundworm => Me/Al
Nemotode => Me/Al
Hookworm => Me/Al
Tapeworm => Praziquantel
Flukes => Praziquantel
Schisto => Praziquantel |
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Term
| What are the three mechanisms of drug resistance? |
|
Definition
(1) Drug doesn't get there, e.g. Gram-negative bacteria have permeable porins, also active efflux of the drug
(2) Drug is inactivated, e.g. bacteria producing beta-lactamases inactivate penicillin, Gram-negative resistance to aminoglycosides via enzymes
(3) Drug is altered, e.g. penicillin binding proteins with altered affinity for drug; mutations in the fluoroquinolone target (DNA gyrase) |
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Term
What are the three forms of recognized antibiotic synergism?
(1 + 1 = 5) |
|
Definition
(1) by blocking sequential setps in a metabolic pathway, e.g. anti-folate TMP-SMX block sequential steps in folic acid pathway
(2) by inhibiting enzymatic inactivation of an antibiotic, e.g. beta lactamase inhibitor + beta lactam antibiotic
(3) by enhancing antibiotic uptake by bacteria, e.g. aminoglycoside + beta lactam antibiotic |
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|
Term
| When are combinations of antimicrobial agents used clinically? |
|
Definition
To treat mixed bacterial infections (i.e. aerobic + anaerobic)
To treat severe infections in hospital setting (i.e. pneumonia)
To achieve a synergistic effect necessary to kill a microbe (i.e. prevent relapses of endocarditis with penicillin + aminoglycoside)
To prevent the emergence of resistance (b/c a microorganism with mutational resistance against two antibiotics is unlikely) |
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Term
| When are antibiotics used in prophylactic prevention of infection? |
|
Definition
To protect healthy individuals from specific infections (gonorrhea, syphillis, anthrax)
To prevent recurrent disease in susceptible patients (frequent UTIs, emphysema, bronchitis, endocarditis)
To protect against infection during "dirty" surgical procedures such as inserting prostheses in immunocompromised pt (give antibiotic before and after surgery, for most likely organism)
To prevent infection of trauma contaminated wounds (animal/human bite wounds) |
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|
Term
| When are antibiotics misused/overused? |
|
Definition
Not for viral infections
Not for fever of undetermined cause
Not in excessive or suboptimal doses
Not as the sole instrument of therapy
Not administered w/o bacterial testing
Not to be taken off course too early |
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Term
Staph. Aureus / Staph. Epidermis:
1st drug choice
2nd drug choice |
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Definition
If infection is sensitive, go with a penicillinase-resistant penicillin (1st) like nafcillin, oxacillin … if that does not work, try (2nd) first generation cephalosporin like cefazolin or cephalexin, TMP-SMX, clindamycin, ampicillin-sulbactam, amoxicillin-clavulanate
If it's MRSA, go (1st) with vancomycin ... if that don't work, try (2nd) TMP-SMX, doxycycline, linezolid, quinupristin-dalfopristin, daptomycin, tigecycline |
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Term
Streptococcus (A, B, C, G, and bovis):
1st drug choice
2nd drug choice |
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Definition
First (1st) try penicillin G or penicillin V or ampicillin
If not, try (2nd) a first generation cephalosporin like cefazolin or cephalexin, then erythromycin, azithromycin, clarithomycin |
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Term
Pseudomonas Aeruginosa:
1st drug choice
2nd drug choice |
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Definition
First (1st) try cefepime, ceftazidime, piperacilli +/- tazobactam, ticarcillin/ticarcillin +/- clavulanate plus an aminoglycoside
If not, try (2nd) ciprofloxacin, levofloxacin, aztreonam, imipenem, meropenem |
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Term
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Definition
Penicillin Antibiotic
Penicillins mimic the structure of transpeptidase enzyme which inhibits subsequent production of highly cross-linked peptidoglycan cell walls, which is critical for bacteria. So penicillins exert their bactericidal effect only on actively dividing cells. They additionally target penicillin-binding proteins necessary for cell shape and cell division. Ultimately activates bacterial autolysins, cell lysis. Often used in combination with an aminoglycoside (e.g. gentamicin) for syngergistic killing.
Active against Gram-negative and Gram-positive cocci (Staph., Strept., Pneumo.), spirochetes of syphillis (Treponema pallidum), and anthrax (Bacillus Anthracis)
Poor oral absorption, so it's administered parenterally. Watch out for resistance. Watch for hypersensitivity reactions. |
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Term
| PENICILLIN V Potassium (V-cillin, Pen-Vee K, et.al.) |
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Definition
Penicillin Antibiotic
More stable and better absorbed than Penicillin G. Less active against most microorganisms, so only used for minor infections. |
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Term
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Definition
Penicillin Antibiotic
Repository form of Penicillin G, slow release at low concentrations. Good for compliance, bad for hypersensitivity reactions.
Penicillin G Procaine used for Strept. Pyogenes infection
Side FX same as penicillin G. Injections can leave bad taste, dizziness, palpitations, visual and auditory disturbances |
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Term
| PENICILLIN G BENZATHINE (Bicillin L-A, Permapen) |
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Definition
Penicillin Antibiotic
Repository form of Penicillin G, slow release at low concentrations. Good for compliance, bad for hypersensitivity reactions.
Penicillin G Benzathine used for Strept. Pharyngitis, Rheumatic Fever, Syphillis
Side FX same as Penicillin G |
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Term
| PENICILLIN G BENZATHINE + PENICILLIN G PROCAINE (Bicillin C-R) |
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Definition
Penicillin Antibiotic
Repository form of Penicillin G, slow release at low concentrations. Good for compliance, bad for hypersensitivity reactions. Taken together, this penicillins can produce a local anesthetic effect, so injections are not painful. |
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Term
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Definition
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Term
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Definition
Penicillinase-Resistant Penicillin
(not used clinically)
with the increase in MRSA
relatively resistant to beta-lactamase
Methicillin also can cause interstitial nephritis |
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Term
| NAFCILLIN (generic, Unipen) |
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Definition
Penicillinase-Resistant Penicillins
Anti-Staphylococcal
Used for serious staphylococcal infections. Because of the increase in MRSA, used less frequently. Still useful for skin infections, soft tissue infections, osteomyelitis, acute endocarditis, Staph. aureus and some Strept. Relatively resistant to beta-lactamase |
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Term
| OXACILLIN (generic, Bactocil) |
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Definition
Penicillinase-Resistant Penicillins
Anti-Staphylococcal
Used for serious staphylococcal infections. Because of the increase in MRSA, used less frequently. Still useful for skin infections, soft tissue infections, osteomyelitis, acute endocarditis, Staph. aureus and some Strept. Relatively resistant to beta-lactamase |
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Term
| What is the drug of choice for MRSA? |
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Definition
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Term
| AMPICILLIN (generic, Polycillin, Omnipen) |
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Definition
Extended Spectrum Penicillin
Greater activity against Gram-negative bacteria (HELPS-ME!). Susceptible to beta-lactamase, so often combined with beta-lactamase inhibitors (e.g. Augmentin)
Side FX same as Penicillin G, can cause rash |
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Term
| AMOXICILLIN (generic, Amoxil, Trimox) |
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Definition
Extended Spectrum Penicillin
Greater activity against Gram-negative bacteria (HELPS-ME!). Susceptible to beta-lactamase, so often combined with beta-lactamase inhibitors (e.g. Augmentin). Amoxicillin is more completely absorbed from GI tract, so lower dose necessary
Side FX same as Penicillin G. Amoxicillin causes less diarrhea than ampicillin, both can cause rash |
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Term
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Definition
The Extended Spectrum Aminopenicillins include coverage against HELPS-ME!
Haemophilus influenza => sinusitis, otitis
Escheria coli => UTIs
Listeria monocytogenes => meningitis, bacteremia
Proteus mirabilis => UTIs
SALMONELLA => typhoid fever, bacteremia, gastritis
Strept. pyogenes/pneumoniae => sinusitis, otitis
Moraxella catatthalis => respiratory tract
Enterococcus faecalis => |
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Term
| TICARCILLIN + CLAVULANATE POTASSIUM (Timentin) |
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Definition
Antipseudomonal Penicillin
Used in combination with beta-lactamase inhibitor (clavK). Used for treating serious infections by Gram-neg and mixed aerobic-anaerobic … Ps. Aeuruginosa in septicemia and UTIs … intra-abdominal or vaginal Bacteroides
Excess sodium in dosage can be problematic (heart failure, renal failure); can affect platelets, prolong bleeding time. |
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Term
| PIPERACILLIN + TAZOBACTAM (Zosyn) |
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Definition
Ureidopenicillin
Used in combo with beta-lactamase inhibitor (Tazo). Broader spectrum of activity than Ticarcillin; useful for treating serious infections caused by Gram-neg and mixed aerobic/anaerobic … community-acquired pneumonia & nosocomial pneumonia (H. influenza, Ps. aeruginosa) ... septicemia (Gram-neg's) ... UTIs in hospital & pelvic inflammatory disease (E. Coli) ... sink infactions (Staph. aureus)
Pipercillin contains less sodium than Ticarcillin, so easier on kidneys; exhibits less prolonged bleeding time than Ticarcillin |
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Term
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Definition
Beta-lactamase inhibitor
used in combo with penicillins
do not work well alone |
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Term
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Definition
Beta-lactamase inhibitor
used in combo with penicillins
do not work well alone |
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Term
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Definition
Other Beta-Lactam Antibiotics
Highly resistant to beta-lactamase. Similar to an aminoglycoside, only effective against Gram-negative rods (E. coli, Klebs. Pneumoniae, Pseud. aeruginosa, S. marcescens, H. influenza, Enterobacter sp.)
Not as much allergic reactions with Aztreonam |
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Term
| IMIPENEM + CILASTATIN (Primaxin) |
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Definition
Carbapenem Antibiotic
Carbapenems, like other beta-lactams, interfere with bacterial cell wall synthesis, cause lysis. THEY ARE VERY RESISTANT TO BETA-LACTAMASE BREAKDOWN. Good use against Gram-positive Strept. & Staph., Gram-negative (N. meningitidis, N. gonnorrhea, Pseudomonas aeruginosa, Enterobacter), anaerobes (B. fragalis). Used for complicated UTIs, serious respiratory tract infections, mixed infections, not for surgical prophylaxis, not for MRSA, not to treat Pseud. infection alone
Should not be used for community-acquired infections, and should be reserved for serious hospital-acquired infections or infections with multiple microorganisms. Imipenem is resistant to beta-lactamase but it does stimulate its production, so be careful. Imipenem can cause seizures |
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Term
| AMOXICILLIN + CLAVULANIC ACID (Augmentin) |
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Definition
Combination Penicillin
Both drugs are well absorbed
The addition of clavulanic acid extends the spectrum
Used for RTIs & UTIs and skin infections (drug of choice) |
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Term
Case Study:
Acute Otitis Media |
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Definition
70% of cases caused by Strept. Pneumoniae (gram-positive cocci) or Haemophilus influenza (gram-negative bacilli) or Moraxella catarrhalis (gram-negative cocci)
44% of cases may be caused by viruses
Tx with Amoxicillin
Then Tx with Augmentin
Then Tx with Cefuroxime; or Cefprozil |
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