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Pharmaco_____: what the body does to the drug (absorption, distribution, elimination.)
Pharmaco_____: what the drug does to the body (local, systemic,cellular).
In terms of drugs, maximal efficacy= _____ effect.
potency- shift of curve to the left and right, right is (more or less potent)
-median effective dose= point at which ____ of the test subjects achieve desired effects pharmacokinetically.
-median toxic dose= point at which ____ of the test subjects are subject to undesireable affects (death).
-Therapeutic Index= (TD50/ED50 or ED50/TD50)
- ceiling effect
- less potent
______: alimentary administration (oral, sublingual, buccal)
______: Non-alimentary administration; more direct, no first pass: inhalation, IV etc.
word bank: Parenteral/Enteral
word bank: urine, liver, adipose
It takes about ___ half life units for the concentration of a medication in the system to leave the body or to reach a steady state. With a half life of twenty four hours, on the fifth day the rate of intake of the drug will equal elimination. If the half life is 12 hours, you will reach a steady in 2.5 days. If you stop taking the drug cold turkey, for the 24 hour half life, it will take __ days to be removed from the body.
_______: component of the cell where a drug binds and initiates a chain of biochemical events.
_______: drug can bind to a receptor and initiate a change in the function of the cell.
_______: drug that will bind to a receptor but will not directly change the function.
______ ______: hunt for the same receptor as the agonist-both the antagonist and the agonist have an equal opportunity to occupy the receptor.
_______ _____: form strong , essentially permanent bonds to the receptors.
_______: amount of attraction between a drug and a receptor.
- competitive agonist
- non-competitive receptor
3 Cell surface receptors:
_____ ____: linked directly to the surface receptors-fastest.
_____ _____: second fastest
____ ______: coupled receptors-meaning it takes a substance on the outside of the cell with the G-protein on the inside of the cell to bind to the receptor.
word bank: G-protein, kinase linked, ion channel
- ion channel
- kinase linked
Basal Ganglia affects _____ functions. (ACH, Dopamine, and GABA)
Reticular formation affects _____ state. (Norepinephrine)
Limbic system affects _____ and _____. (ACH and dopamine)
- mood and emotions
Blood brain barrier acts as a selective filter and seems to protect the CNS by limiting harmful substances that enter into the brain and SC; generall (non-polar or polar; lipid or non-lipid soluble) drugs are able to cross. 2nd generation antihistamine drugs are less lipid soluble therefore they are (more or less) likely to cross.
non-polar, lipid soluble
Second generation antianxiety drugs have less side effects because they prefer (alpha 1 or alpha 2) receptors which mediate sedation without side-effects.
Alpha 1 (and were talking about nonbenzodiazipines)
_____-_____: used to both relax the patient and promote sleep. At higher doses, hypnosis and even general anesthesia.
(Benzodiazepines or Barbiturates) are preferred to treat anxiety/depressive disorders however neither should be used for prolonged periods.
-Tricyclic antidepressants block the _____ of NT's (dopamine, NE, and serotonin).
-Monoamine oxidase inhibitors block the enzymes that ______ NT's.
- ______-generation antidepressants are more selective for blocking serotonin/NE reuptake and have less side-effects.
Monoamine oxidase inhibitors have dietary restrictions which can lead to excessive catecholamine levels and a ______ crisis. Trcyclics can cause ______ ______, and all 3 classes of antidepressants exhibit anticholinergic symptoms which are?
- orthostatic hypotension
- dry mouth, constipation, urinary retention, blurred vision
______: (schizophrenia) characterized by distrubed thought processes (delusions/hallucinations), and the positive symptoms are caused by overactivity of _____ in the limbic system, and the negative symptoms may also be attributable to decrease of ______ in higher areas of the brain.
Antipsychotic drugs work by blocking _____ receptors especially (D1 or D2)?
Antipsychotic drugs have motor and non motor side effects; of all the motor symptoms, _____ _____ symptoms are the hardes to alleviate and are usually the last ot show up.
CNS related side effects of antiseizure medications as a whole are usually a result of inadvertent effects in the _________.
These drugs try to inhibit firing of cerebral neurons by increasing (excitatory/inhibitory) effects of GABA and by decreasing the (excitatory/inhibitory) effects of amino acids. Side effects include: sedation, ataxia, nystagmus, GI distress, and dizziness.
What are the three main criteria patients should meet in order to be good candidates for slow withdrawal from antiseizure medications.
1. Free of seizures for the last __ years while on meds.
2. having a ____ neurological exam prior to withdrawal.
3. (young/old) when the seizures started.
In parkinson's, _______ producing cells in the substantia nigra begin to degenerate, leaving the cholinergic pathway to dominate and ____ to begin in the hands.
________: resolves dopamine deficiency by being converted to dopamine after crossing the BBB. Following absorption, it is converted to dopamine by dopa decarboxylase. ______ is a peripheral decarboxylase inhibitor that prevents peripheral decarboxylation (decreases the amount of medication needed).
______ toxicity may present as sudden onset of bizarre movement symptoms in patients, such as facial grimmacing, twitching, and tongue protrusion. The pt may also exhibit strange leg movements and appear overly restless and excited.
General anesthetics are typically given by injection or inhalation. Inhalation of anesthetics are primarily stored in the ____ and excreted through the lungs.
True or False: both general anesthetic and neuromuscular blocker can cause anesthsia by themselves.
false; neuromuscular blockers can't by themselves, only stop movement
Local anesthetics work by ______ action potential propogation along neuronal axons, which is believed to occur from the anesthetic molecule inhibiting the opening of membrane _____ channels.
_____ diameter fibers seem to be the most sensitive to anesthetic effects with prossiver ____ fibers being affected as anesthtic concentration increases.
________ agents such as epinephrine can be given in conjunction with local anesthetics so that washout and sytemic absorption of the local anesthetic can be avoided.
- The primary advantage of local anesthtic admin by iontophoresis and phonophoresis is that ___ skin breakage is required.
____phoresis: effects can be enhanced by electrical current.
___phoresis: can be enhanced by US
_____ _____: often result from peripheral injury or condition that affects the muscles or peripheral components of the neuromuscular apparatus. Located in a specific area, not velocity dependant, involuntary, and continuous RX: diazepam and polysynaptic inhibitors.
_______: CNS injury or condition and generalized; velocity dependent. RX: bacolfen, diazepam, and dantrolene sodium.
______ application of balcofen is administered in the subarachnoid space surrounding hte specific level of the spinal cord and allows for increased drug effectiveness with smaller doses.
Botulinum toxin wears off after awhile because new (pre or postsynaptic) terminal s sprout.
Opiod receptors: mu, kappa, and delta. Which one is primarily responsible for analgesic effects?
In general, SE's include sedation, consitipation, orthostatic hypotension, and euphoria.
Two advantages of mixed opioid agonists/antagonists:
-produce adequate analgesia with (more or less) risk of side effects associated with Mu opiods.
- (more or less) addictive characteristics of the stong mu receptor agonists such as morphine.
______: opioid antagonist used for opioid overdose. It should have no effects on someone who hasn't taken opioids. Respiratory depression is a serious side effect of opioid overdose.
______: the need for more of a drug to achieve a given effect.
______ _____: onset of withdrawal symptoms if a drug is suddenly discontinued.
______ _____: seems to create drug seeking behavior that causes the addict to relapse into use of the drug long after the physiologic effects.
- physical dependane
- psychological dependance
_____: relieve mild to moderate pain.
_____: decrease body temp
______: decrease inflammation
______: decrease blood clotting
Which two effects do acetaminophen exhibit?
- (analgesic and antipyresis)
NSAIDs inhibit COX-1 and COX-2 enzymes:
COX-_: synthesize prostaglandins in the stomach that help protect from the stomach acid.
COX-_: emergency enzyme which is produced in response to injury.
Beneficial effects of NSAIDs come from inhibition of COX-__.
Unwanted effects usually comes from inhibition of Cox-_ which results in increased GI acid and decreased renal function.
Aspirin inhibits COX1 and COX2? True or False
COX-2 inhibiotrs were removed from the market for the potential risk of _____ _____ and stroke. (celebrex is still on the market.)
3 general characteristics of RA:
- 1. pain
- 2. stiffness
- 3. inflammation (hands, feet and progressing to larger joints)
Why is acetaminophen the best choice for RA. This reason is the same for why it is better for OA.
they lack the anti-inflammatory effects
_______: extremely effective for anti-inflammatory agents. good for high dose/ short term useage for acute axacerbations of RA. However long term use can cause serious musculoskeletal problems.
SE's of glucocorticoids:
Exert a general catabolic effect on all types of supportive tissues, ______ bone loss in patients with arthritis when drugs are used at higher doses for long duration. Can also cause muscle _____.
DMARD stands for: _____ _____ ____ ____
-used to control synovitis and erosive changes during the active stages of rheumatoid joint disease.
-attempts to reduce remission by modifying the pathologic process inherent to RA.
-inhibit certain aspects of the immune response thought to be unerlying rheumatoid disease.
disease modifying antirheumatic drugs
General classes of DMARDS:
______ drugs: used for their effects on the immune system.
______ ______: used to affect immune system but take a long time to act.
______ ______ factor: inhibitors mostly affect their inflammatory process.
- anticancer drugs (organ rejection)
- gold compounds
- tissue necrosis factor
Adrenergic receptors (autonomic pharm)
_____ _: primary action to constrict blood vessels
_____ _: primarily CNS negative feedback to inhibit alpha 1 type effects (decrease NE release)
_____ _: most in heart to increase rate and force of contraction.
_____ _: mostly bronchioles to open the airways; also relax the gall bladder and uterus.
- alpha 1
- alpha 2
- beta 1
- beta 2
Drugs that affects nicotinic cholinergic receptors will affect activity in the ______ and _____ divisions of the ANS. This is because the receptors are located on the junction between ___ and ___ ganglionic neurons in the pathways.
- sympathetic and parasympathetic
- pre and post ganglionic
_____ acting: bind directly to the cholinergic receptor to activate it, which in turn initiates a cellular response. These stimulants may be considered true cholinergic agonists. Used to treat the decrease in smooth muscle tone following abdominal surgery or trauma. Limited to topical applications due to adverse effects.
______ acting: stimulants that increase activity at cholinergic synapses by inhibiting the acetylcholinesterase enzyme. This enzyme is normally responsible for destroying acetylcholine after this NT is released from the presynaptic terminal. Used for glaucoma, myasthenia gravis, AD, and overdose.
- Direct acting
- Indirect acting
______: prototypical anticholinergic drug and blocks muscarinic activity. Used to treat extremely high blood pressure, and sometimes an adjunct in general anesthesia.
Anticholinergic drug side effects: 5
dry mouth, blurred vision, urinary retention, constipation, and tachycardia
Alpha-__ agonist are used most therapeutically for vasoconstrictive properties. Treats high blood pressure. headache, slow heart rate, chest pain etc. May cause reflex bradycardia.
Alpha-__ agonists are generally _____ to induce bronchodilation, or can be taken orally to help prevent preterm labor.
Alpha-_ receptor antagonists can be used to _____ blood pressure. The most prominent side effect is reflex tachycardia
- alpha-1 decrease
Alpha 2 blockers are not used frequently for human treatments except to _____ the effects of alpha-2 stumulants.
______ (blockers or) antagonists are used primarily for treating: hypertension, angina pectoris, cardiac arrhythmias, and MI.
Diuretics increase excretion from the kidneys by removing _____ from the body, resulting in decreased fluid volume in the body. Could potentially cause an electrolyte imbalance and excessive fluid loss.
_____ blockers decrease vascular resistance.
Alpha-_ agonists combat HTN by inhibiting sympathetic discharge form the brainstem's vasomotor center.
_____ blockers: clock nicotinic ANS receptors.
_____ channel blocker: reduce calcium entry into vascular smooth muscle and cardiac stirated muscle cells yielding decreased BP, HR, and contractility.
_____ _____: work as donors of the nictric oxide. Cardiac work is thus decreased from both the venous and arterial sides of the heart, and it further helps that coronary arteries also dilate.
______: exhibits a significant first pass effect, one reason why fast acting tabs are given sublingually to treat angina. No more than __ doses administered five minutes apart.
- organic nitrates
Nitrates (increase or decrease) myocardial demand primarily via peripheral vasodilation. Beta blockers lead to (increased or decreased) myocardial demand (directly or inderectly) on the heart. Calcium channel blockers lead to (increased or decreased) myocardial demand via peripheral vasodilation and (increased or decreased) myocardial oxygen supply.
True or False: increased arrhythmias may actually occur as a result of using antiarrhthmic drugs?
Know that when you see patients being treated for heart failure, be looking for signs of acute congestive heart failure that may occur due to drug side effects or lack of current therapy (coughing, dyspnea, rales and frothy sputum).
seriously, know it
______: drug commonly used to treat heart failure via positive inotropic effects, and that most other classes of drugs used to treat heart failure are used to ability to (increase or decrease) cardiac workload.
_____ inhibitors: known to be one of the only classes of drugs that may actually increase life expectancy of CHF patients.
Tissue plasminogen activator catalyzes conversion of plasminogen to plasmin which _____ the clot.
_______: inhibit platelet aggregation and platelet induced clotting; used for venous clots. Should not be used to treat hemorrhagic stroke.
_______: help dissolve an already existing clot, arterial or venous.
Warfarin therapy: used to cause anticoagulation by inhibiting regeneration of vitamin-_ dependent clotting factors.
-Primary problem with 1st generation of antihistamines is _____.
-Cromones are used to (prevent or treat) inflammatory responses in the respiratory tract due to their stabalizing effect on mast cells in the the tissue.
- Leukotriene inhibitors block the enzyme lipoxygenase to decrease leukotriene production and helps (increase or decrease) the inflammatory response.
_____ _____ ____ (PUD) is generally treated with antacids, H2-blockers, and proton pump inhibitors.
peptic ulcer disease
Although antacids neutralize stomach acids, overuse can cause an acid-rebound effect whereby drug discontinuation leads to worse acid production than before.
that is a problem
-digestants aid in _____.
-emetics promote _____.
- antiemetics prevent ______.
- cholelythic drugs help dissolve ______>
- vomiting (and nausea)