Term
|
Definition
| Calcium influx lead to vesicle fusion and neurotransmitter release |
|
|
Term
|
Definition
| Most common excitatory synapse, synthesized from glutamine in nerve terminal mitochondria |
|
|
Term
|
Definition
| Glutamate action; permeable to Na, K, and Ca; requires glutamate/glycine binding for action |
|
|
Term
|
Definition
| Type 1 = increase IP3, type 2/3 = decrease cAMP via adenylyl cyclase |
|
|
Term
|
Definition
Most inhibitory synapses in CNA, receptors make permeable to Cl.
Pre-synap = inhibit Ca conduction, decreasing release and increase K conduction, hyperpolarizing and decreasing Ca influx
Post-synap = increase K conduction=> hyperpolarizes |
|
|
Term
|
Definition
| Synthesized from tyrosine, catabolized by MAO, inactivated vy COMT |
|
|
Term
|
Definition
| Synthesized from dopamine, catab by MAO, inactive by COMT, all G-protein receptors |
|
|
Term
|
Definition
| Made from tryptophan, catab by MAO, implicated in depression, anxiety, stress, schizophrenia, hallucinations, OCD, substance abuse, migraine, sleep, temp/endocrine control |
|
|
Term
|
Definition
Anandamide, 2- arachidonylglycerol
Not stored in vesicles, rapidly synth after depolarization, can act as retrograde transmitters, activate pre-synaptic terminal recpetors;
Inhibit adenylyl cyclase and Ca conduction; implicated in memory, cognition and pain perception |
|
|
Term
|
Definition
| Synthesized in CNS neurons, mainly in ventral posterior hypothalamus which projects diffusely. |
|
|
Term
|
Definition
| lipid soluble, non-polar molecules can diffuse passively across the BBB or enter the brain by transporters which are carrier mediated; less prominent in the hypothalamus and MUCH less effective in median eminence, area postrema, pineal, subfornical organ and subcommisural organ. |
|
|
Term
| Cellular (pharmacodynamic) tolerance |
|
Definition
| desensitization of recpetors |
|
|
Term
| Metabolic (pharmacokinetic) tolerance |
|
Definition
| induce the expression of degradation.metabolism molecules |
|
|
Term
|
Definition
| reduce anxiety and relax/calm |
|
|
Term
|
Definition
| produce drowsiness and bring on sleep |
|
|
Term
|
Definition
| fail to initiate the breathing response; DO NOT PRESCRIBE HYPNOTICS (may decrease arousal response to hypoxia and reduce airway tone) |
|
|
Term
| Circadian rhythm disturbances |
|
Definition
| hypnotics help reset the clock |
|
|
Term
| Medication induced insomnia |
|
Definition
| alcohol, SSRI, anti-Parkinson's, methylxanthines, diuretics |
|
|
Term
|
Definition
| difficulty starting/continuing sleep for >1 month with impairment of awake function unrelated to other illness |
|
|
Term
|
Definition
Sedative Hypnotic, Increase GABA-induced Cl channel opening=> hyperpolarization; High doses= GABA receptor activation, inhibit nAChR autonomics and muscle
Death = depression of respiration/CV function |
|
|
Term
|
Definition
| Low therapeutic index, doesn't induce physiologic sleep (dec. onset/# wakes,limits deep and REM sleep), significant interactions, abuse/addiction potential, induces liver P450, , cross tolerance to other depressants, withdrawl (phenobarbitol and taper off slowly to treat) |
|
|
Term
|
Definition
| long acting barbiturate, antiseizure agent, used for hypnosedative withdrawl, half=80-120 hrs |
|
|
Term
|
Definition
| Intermediate acting barbiturate, hypnotic, preoperative sedative, half=15-50 hrs |
|
|
Term
|
Definition
| Short acting barbiturate, induce/maintain anesthesia, half=8-10 hrs |
|
|
Term
|
Definition
| Liver, then kidney; up to 30% excreted unchanged in urine; intoxication resembles alcohol intox, severe = coma, hypothermia, hypotension, bradyapnea, possible early tachycardia then btadycardia=> shock |
|
|
Term
|
Definition
Supportive care, treat shock with respirations; remove drug (vomit, lavage, charcoal, hydrate, alkaline urine)
Most deaths from cardiovascular collapse, resp. complications and renal failure
NEVER GIVE CNS STIMULANTS |
|
|
Term
| Benzodiazepine site ligands |
|
Definition
| End in -lam and -pam; higher therapeutic index, lower toxicity, not general CNS depressant; allosterically enhance GABA binding and Cl opening; DO NOT COMBINE WITH ALCOHOL |
|
|
Term
|
Definition
|
|
Term
|
Definition
| Librium, benzo for anxiety, alcohol withdrawal, preanesthetic |
|
|
Term
|
Definition
| benzo for seizures, mania, movement disorders, 1/day |
|
|
Term
|
Definition
| Valium, benzo for anxiety, status epilepticus, muscle relax, preanesthetic; half = 43+/-13 hrs |
|
|
Term
|
Definition
| benzo for insomnia, very long lasting due to multiple metabolites (74+/-24 hrs) |
|
|
Term
|
Definition
| benzo for anxiety, status epilepticus, preanesthetic |
|
|
Term
|
Definition
| benzo preanesthetic, intraoperative medication; very short acting (2 hrs) |
|
|
Term
|
Definition
|
|
Term
| Benzodiazepine adverse effects |
|
Definition
| Impaired mental/motor f'n, ataxia, residual daytime desation, anterograde amnesia; additive with CNS depressants (alcohol); abrupt withdrawal= anxiety, nausea, seizure, rebound insomnia |
|
|
Term
|
Definition
| Rohypnol, benzo date rape drug for amnesia and sedation |
|
|
Term
|
Definition
| distribute to high perfusion regions first (brain), metab in liver to active metabolites, interact with P450 3A4 inhibitors |
|
|
Term
|
Definition
| =>desmethyldiazepam (active, 40-100)=>oxazepam (active, 3-21)=>conjugation (lorazepam immediately conjugated)=>excretion |
|
|
Term
|
Definition
| Z-drugs; hypnotics, non-anxiolytic.relaxant/antiseizure, less rebound insomnia |
|
|
Term
|
Definition
| Ambien, non-benzo, increase sleep duration, short term use only, withdraw can anxiety, tremor, agitation, rebound insomnia and seizures; abuse possible, ~8hr effect |
|
|
Term
|
Definition
| Sonata; decreased sleep latency (~4hrs), short term use only |
|
|
Term
|
Definition
| Lunesta; increase sleep duration, long term use OK, low abuse potential |
|
|
Term
| Non-benzo adverse effects |
|
Definition
| headache, additive with CNS depressants, morning sedation if used late at night (8 hr action), may be psycho habit forming, sleep walking/eating, amnesia |
|
|
Term
|
Definition
| Benzo/non-benzo competitive antagonist; decreases recovery time; rapid onset, short half-life (need multiple doses to overcome other drug); adverse= agitation, confusion, dizzy, nausea, cross-rxn with other brain substances |
|
|
Term
|
Definition
| serotonin derivative from pineal, activated by light, suppress ovarian f'n, role in biological rhythms |
|
|
Term
|
Definition
| Melatonin receptor agonist, MT1 (sleepy) and 2 (circ. rhythm) in suprachiasmatic nucleus; hypnotics (fall asleep), interact with P450 1A2 inhibitors, no CNS depression, no motor/cognitive impair; adverse = increased prolactin |
|
|
Term
|
Definition
| Not sleep related; reduce anxiety, depression and many psych disorders; low abuse potential, slow onset, substantial number of non-responders |
|
|
Term
Diphenhydramine
Doxylamine |
|
Definition
| OTC sleep aids; antihistamines, not consistently effective; rapid tolerance, may have residual daytime sedationand anti-cholin. effects |
|
|
Term
|
Definition
| dietary supplement, helps sleep disorders? |
|
|
Term
|
Definition
| dietary supplement, helps sleep disorders? |
|
|
Term
| Gamma-hydroxybutyrate/sodium oxybate |
|
Definition
| GABA precursor, act as CNS depressant; GHB=controlled substance, very addictive (euphoria, hallucin, date rape), SO=scrip only, treats narcolepsy; abuse = amnesia, vomit, resp/CV depression, loss conscious, seizure, death; as prescribed = confusion, headache, nausea, vomit, dizzy, urine incontinence |
|
|
Term
|
Definition
| stimulant, inhibit NE and DA uptake, treat narcolepsy and excessive sleepiness; low abuse no crash or high, side effect=headache (overstim); induces P450, increases contraceptive/carbamazine/cyclosporin metab, decreases diazepam/propanolol/phenytoin metab |
|
|
Term
|
Definition
| spasmolytic, GABA-B receptor agonist, increase K perm/inhib Ca influx; adverse = drowsy, seizure, pump implant can cause CNS depression |
|
|
Term
|
Definition
| Central alpha2 receptor agonist, increase pre/post motor inhibition; adverse=drowsy, hypotension, dry mouth, weakness |
|
|
Term
|
Definition
| Decrease Ca release from sarcoplasmic retic., direct muscle action; adverse=general weakness, sedation; treat malignant hyperthermia (NMJ block) |
|
|
Term
|
Definition
| transient episode of brain dysfunction from rhythmic, synchronous neuronal firing |
|
|
Term
|
Definition
| group of chronic disorders with recurrent seizures |
|
|
Term
|
Definition
| PRESERVATION OF CONSCIOUSNESS, sensory auras, limited unilateral motor convulsions |
|
|
Term
|
Definition
| impaired consciousness, automatisms, confusion and lethargy |
|
|
Term
| Partial seizure secondarily to generalized |
|
Definition
| starts off partial, then becomes complex (1-2 minutes) |
|
|
Term
|
Definition
| CARBAMAZINE, PHENYTOIN, OXCARBAZEPINE, LAMOTRIGINE, VALPROATE, Topiramate, Gabapentin, levetiracetam, zonisamide, tiagabine, phenobarbital, pregabalin, felbamate |
|
|
Term
| Tonic-Clonic seizures (grand mal) |
|
Definition
| LOC, tonic spasm of body, prolonged post-ictal stupor |
|
|
Term
| Absence sizure (petit mal) |
|
Definition
| Abrupt interruption of consciousness assoc. with staring and cessation of ongoing activities; mild jerking, LACK OF POST-ICTAL ABNORMALITIES |
|
|
Term
| Generalized seizure drugs |
|
Definition
| VALPROATE, PHENYTOIN (GM), CARBAMAZEPINE (GM), ETHOSUXIMIDE (PM), Lamotrigine (GM), topiramate (GM), levetiracetam (GM), oxcarbazepine (GM), phenobarbital (GM), zonisamide (PM), levetiracetam (PM) |
|
|
Term
|
Definition
Inhibit Na channels, high protein binding;
adverse= gum hyperplasia, hirsutism, coarse face feature, endocrine abn., teratogen |
|
|
Term
|
Definition
Related to tricyclic antidepress; inhibit Na channels, decrease synaptic transmission, induce own liver metab; adverse=liver damage, mild persistent leukopenia, rare aplastic anemia/agranulo/hyponat/teratogen/osteoporosis
REQUIRES LIVER F'N TESTS |
|
|
Term
|
Definition
| Good safety profile; inhibit Na and high voltage Ca channels, enhance K currents; prodrug, less liver enzyme induction with few adverse effects (hyponatremia, Stevens Johnson syndrome, toxic epidermal necrolysis, multi-organ hypersens), decreases T4 |
|
|
Term
|
Definition
| Positive GABA-A receptor modulator, decrease glutamatergic transmission; used in INFANTS, adults=sedation |
|
|
Term
|
Definition
GABA amino acid analog; Decrease Ca influx, excretes unchanged;
adverse= periph edema, behavior/thought disorders age 3-12; similar to high dose diazepam |
|
|
Term
|
Definition
GABA uptake inhibitor, highly protein bound, liver metab;
adv= SEIZURES, non-convulsive status epilepticus in non-epileptics |
|
|
Term
|
Definition
Inhibit delayed K channel, inhibit N-type Ca channel;
adv= irritability, behavior change, halluc, psychosis |
|
|
Term
|
Definition
Inhibit NMDA receptors, enhance GABA transmission;
adv=APLASTIC ANEMIA, SEVERE HEPATITIS/FAILURE; LIVER F'N TESTS REQUIRED |
|
|
Term
|
Definition
Only for Absence seizure, Inhibit T-type Ca channel;
adv= blood dyscrasias, skin rxn, Parkinsonian symptoms, photophobia |
|
|
Term
| Valproic acid/ sodium valproate |
|
Definition
Inhibit Na channel, T-type Ca channel and GABA transaminase; stim GABA synthesis via GAD;
adv= HEPATOTOXICITY, pancreatitis, TERATOGEN, thrombocytopenia, hyperammonia, osteoporosis; LIVER F'N TEST REQ'D |
|
|
Term
|
Definition
| Inhibit Na channels/glutamate release; used for Lennox-Gastaut syndrome ONLY; adv= STEVENS JOHNSON SYNDROME, arthritis, hypersensitivity, multiorgan failure |
|
|
Term
|
Definition
Inhibit Na channel, enhance GABA transmission, activates hyperpolarizing K cahnnel;
adv= metab acidosis, severe myopia/glaucoma, hypohidrosis, hyperthermia, language dysfunction |
|
|
Term
|
Definition
Sulfonamide derivative; inhibit Na/T-type Ca channels, weak carbonic anhydrase inhibitor;
adv=allergic rxn to sulfonamides, hypohidrosis, hyperthermia (kids), photosensitivity, irritability |
|
|
Term
|
Definition
Used in INFANTILE SPASMS; Irreversible GABA degradation inhibitor;
CONTRA=MENTAL ILLNESS (may cause psychosis), adv=long-term visual field distrubances |
|
|
Term
| Oral contraceptive interactions |
|
Definition
| Carbamazepine, felbamate, lamotrigine, Oxcarbazepine, phenobarbital, phenytoin, topiramate |
|
|
Term
|
Definition
continuous, prolonged seizure (5-10 minutes), most often tonic-clonic, requires cardio/resp/metab management;
Drugs=LORAZEPAM, DIAZEPAM, FOSPHENYTOIN |
|
|
Term
|
Definition
myoclonic spasms, 1st attack before year 1;
Drugs=CORTICOTROPIN (ACTH), PREDNISONE |
|
|
Term
|
Definition
| NOT epilepsy, brought by fever in kids; NO MEDS |
|
|
Term
| Antiseizure therapy issues |
|
Definition
| Many have low therapeutic index; adv= sedation, dizziness, ataxia, headache, tremor, cognitive impairment, behavioral/psychiatric changes, nervousness, weight change, nausea, vomit |
|
|
Term
| Seizure therapy termination |
|
Definition
| If seizure free for 2 years, consider termination, relapse between 25-50%; high risk of status epilepticus with abrupt withdrawl |
|
|
Term
|
Definition
| controlled reversible state of analgesia, amnesia, LOC, sensory/autonomic reflex inhibition, skel mm relaxation |
|
|
Term
|
Definition
| use of several drugs to achieve a state of general anesthesia |
|
|
Term
| Minimum alveolar concentration |
|
Definition
| steady state minimum concentration of an inhalational agent to immobilize 50% of subjects |
|
|
Term
|
Definition
| 1.3 MAC, 95% of patients will not move at incision |
|
|
Term
|
Definition
| analgesia w/o amnesia, impaired judgement, vertigo/ataxia, increased respiration, blood pressure, heart rate |
|
|
Term
|
Definition
| delirious, excited, amnestic. Irregular respirations, struggling and retching |
|
|
Term
| Stage of Surgical anesthesia |
|
Definition
| Recurrence of regular respirations to cessation of spontaneous resipration. BP drop, relaxation, loss of corneal reflexes. |
|
|
Term
| Stage of medullary depression |
|
Definition
| cessation of spontaneous respirration; support needed or they'll die |
|
|
Term
|
Definition
| relative affinity for blood compared to air; low solubility requires relatively few molecules dissolved into the blood to equilibrate pressures; low solubility = faster onset |
|
|
Term
|
Definition
| speed of induction can be increased by increasing concentration |
|
|
Term
|
Definition
| Increasing ventilation generally increases the speed of induction |
|
|
Term
|
Definition
| Increased flow = slower induction (more blood to saturate to increase pressures |
|
|
Term
|
Definition
| Released in the lungs, least soluble eliminated most quickly |
|
|
Term
| Inhalational pharmacodynamics |
|
Definition
| Increase threshold for neuron firing with a decrease in neuronal activity; increase glycine ability to activate Cl channels=> inhibition at level of the spinal cord/stem; |
|
|
Term
|
Definition
| All potent volatile agents reduce consumption |
|
|
Term
| Respiratory inhalational effects |
|
Definition
| Decreased tidal volume and increased respiratory rate; all agents decrease ventilatory response to increased PaCO2 |
|
|
Term
| Inhalational Renal effects |
|
Definition
| Decreased renal blood flow, decreased glomerular filtration rate, and probable impairment of renal autoregulatory mechanisms |
|
|
Term
|
Definition
| inherited, hypermetabolic activity, marked carbon dioxide production, altered skeletal muscle tone, and metabolic acidosis; altered intracellular calcium regulation; treat with dantrolene |
|
|
Term
|
Definition
| Most widely used worldwide; cheap; high solubility (need high dose), prominent heart depression, induced arrhythmias |
|
|
Term
|
Definition
| Most used in modern countries; cheap, low solubility; airway irritation, vasodilation, HR increases |
|
|
Term
|
Definition
| low solubility, fast onset, much like isoflurane; expensive, vasodilation with decreased MAP, increased HR |
|
|
Term
|
Definition
| low solubility (fast on/off), well tolerated, no HR change; expensive, vasodilation and decreased cardiac output |
|
|
Term
|
Definition
| Minimal myocardial/vascular effects, low solubility; not potent, increased ICP and cerebral blood flow |
|
|
Term
|
Definition
| highly protein bound and highly lipid soluble |
|
|
Term
|
Definition
| Profound CNS depression via GABA-A enhancement; rapid BBB crossing, venodilation decreases preload, potent respiratory depressant, cerebral metabolic O2 consumption/blood flow decreased=> ICP decrease |
|
|
Term
|
Definition
| Profound CNS depression via GABA enhancement; minimal cardio/resp effects, rapid onset/recovery; limited by potential adrenocortical suppression; post-operative nausea and vomiting |
|
|
Term
|
Definition
| CNS depression via GABA-A enhancement; similar to barbiturates, more rapid recovery; profound resp depressant, decreased MAP secondary to decreased syst vasc resistance; rapid clearance and extrahepatic metabolism; amnestic and anti-emetic, no analgesic properties |
|
|
Term
|
Definition
| Act at central/peripheral mu/kappa/delta receptors; ANALGESIC, minimal circulatory deterioration; potential chest wall rigidity; treat with naloxone |
|
|
Term
|
Definition
| GABA-A receptor mediated inhibitory neurotransmission; ANXIOLYTIC/AMNESTIC; Midazolam most common, water soluble, short half-life; Antagonist=flumazenil |
|
|
Term
|
Definition
| Inhibitor of glutamic acid excitation at NMDA receptor; phencyclidine derivative, produces dissociative anesthesia, catatonia, amnesia, analgesia; cardio stimulant by secondary sympathomimmetic activity; catecholamine reuptake decrease; increased cerebral blood flow/metabolism |
|
|
Term
| Clinical local anesthetic makeup groups |
|
Definition
| Lipophilic (aromatic ring), intermediate chain, hydrophilic group; increased hydrophobicity = increases anesthetic potency/duration/toxic side effects |
|
|
Term
|
Definition
| Nerve conduction blockade, vasoconstriction, inhibit catecholamine uptake; primarily topical anesthetic in upper resp tract |
|
|
Term
|
Definition
| prototype ester local anesth, low potency, short duration, can inhibit action of sulfonamides |
|
|
Term
|
Definition
| greater potency, longer duration |
|
|
Term
|
Definition
| topical use only, often directly applied to wounds/ulcers; used in OTC topicals, long duration due to low water solubility |
|
|
Term
|
Definition
| Amide type; Greater potency, longer duration, widely used; antiarrythmic agent |
|
|
Term
|
Definition
| amide type; greater potency, longer duration than lidocaine, more cardiotoxic than lido |
|
|
Term
|
Definition
| weak bases, predominantly charged at physiologic pH; binding site only accessible on cytoplasmic side; uncharged crosses the membrane, becomes charged, acts on Na channel; selectively blocks sodium permeability, stopping conduction |
|
|
Term
|
Definition
| Nerves w/o myelin/little myelin blocked first; sensory nerves lost pain, temp, touch, deep pressure, motor; nerves on outer part of bundle blocked before inner part |
|
|
Term
| Local anesthetic metabolism |
|
Definition
vasoconstrictor addition leads to slower absorption/prolong action duration; ester type hydrolyzed very rapidly by plasma cholinesterase; amide type metab by liver P450; Ester metabolites inhibit sulfonamide antibiotics
Adv=hypersensitivity rxns from PABA metabolites |
|
|
Term
| Local anesthetic reactions |
|
Definition
| CNS=stimulation, seizures, depression, death |
|
|
Term
| Cardiovascular local anesthetic effects |
|
Definition
| decrease electrical excitability, conduction rate, BP and contraction strength; |
|
|
Term
|
Definition
| increased activation of DA in mesolimbic pathways; enlarged heart, paranoia, psychotic behavior, nasal septum damage; withdrawal=ahedonia, increased appetite, lethargy, chronic depression, sexual dysfunction |
|
|
Term
| Injectable local anesthetics |
|
Definition
| articaine, chlorprocaine, mepivacaine, prilocaine, ropivacaine |
|
|
Term
| mucous membranes/skin local anesthetics |
|
Definition
| diclonine hydrochloride, premoxine hydrochloride |
|
|
Term
| Opthalmologic local anesthetics |
|
Definition
|
|
Term
|
Definition
| reversible block of sodium permeability; works on outer mouth of Na channel |
|
|
Term
| Parkinson's disease symptoms |
|
Definition
| akinesia, tremor, rigidity, alteration of posture, mask face, shuffling gait, loss of associative movement, hypersalivation; pill rolling, worse when relaxing; cogwheel resistance; need 70% loss before symptoms |
|
|
Term
|
Definition
| Exerts inhibitory tone on cholinergic interneurons and GABAergic neurons w/in the striatum; inhibit release of ACh which stimulates GABAergics; directly inhibits GABAergic efferent firing; |
|
|
Term
|
Definition
| L-Dopa; can cross BBB, gets metabolized to dopamine inside brain; most gets metabolized peripherally, need to be increased and gradually to effective levels; reduces bradykinesia and rigidity |
|
|
Term
| L-dopa side effects, early |
|
Definition
| nausea (area postrema), orthostatic hypotension (stim presynapt symp receptors block NE release, prevent arteriolar restrict), arrythmias (beta stim) and psychotic behavior (halluc/delusions in mesolimbic system) |
|
|
Term
| L-Dopa side effects, late |
|
Definition
| dyskinesia (faciolingual tics, bobbing/rocking) from on/off phenomenon, depression, anxiety, insomnia, euphoria, hallucination, nightmares |
|
|
Term
|
Definition
| Interact with MAOI's (cause hypertensive crisis); arrythmias should be given as last resort; antipsychotics antagonize L-dopa |
|
|
Term
|
Definition
| decarboxylase inhibitor that can't enter brain, prevents peripheral degredation of L-dopa before it can enter brain, lets lower doses be given; early side-effects gone, late ones still there (maybe worse); Sinemet= mix 10:1 ldopa to carbidopa |
|
|
Term
|
Definition
| MAO-B inhibitor, decreases dopa breakdown in the brain without catecholamine buildup in peripheral tissue; no hypertensive crisis |
|
|
Term
|
Definition
| COMT inhibitor; prevent l-dopa breakdown, less needed to get effect |
|
|
Term
Bromocriptine
ropinirole
pramipexole
rotigotine (transdermal) |
|
Definition
dopa agonist; adv=nausea, hypotension, dyskinesia, hallucination, delusion;
Bromo + l-dopa = limits on-off phenom |
|
|
Term
Benztropine
trihexphenidyl |
|
Definition
| anti-cholinergic drugs, reduce tremor in Parkinson's; adv=dry mouth, blurry vision, urinary retention |
|
|
Term
|
Definition
| antiviral, improve Parkinson symptoms by being dopa releasing agent; not as good as l-dopa, better than antimuscarinics alone |
|
|
Term
| Drug selection recommendation |
|
Definition
Rasagiline may delay symptom onset in newly diagnosed
1st = Agonist (rotigotine, pramipexole, ropinirole)
2nd = Add L-dopa and carbidopa
3rd = COMT inhibitors with L-dopa
4th = add atypical antipsychotic to combat l-dopa hallucinations |
|
|
Term
Donepezil
rivastigmine
galantamine |
|
Definition
| acetylcholinesterase inhibitros, CNS selective; adv=nausea, vomit, diarrhea, abd pain, anorexia; used in alzheimers |
|
|
Term
|
Definition
| NMDA receptor antag, neuroprotective in alzheimers, slows progression |
|
|
Term
|
Definition
| likely to be genetic than enviro; lack initiative, disinterest, limited affect = neuroleptic syndrome |
|
|
Term
antipsychotics
chlopromazine
haloperidol |
|
Definition
| block dopamine receptors; don't cure it, just treat it; takes hours to weeks; adv from block ACh and alpha receptors on top of dopa block |
|
|
Term
| antipsychotic non-neuro side effects |
|
Definition
| orthostatic hypotension (alpha 1 block), altered sexual dysfunction (alpha block), decreased prolactin (block dopa), weight gain, sedation (most with chlorpro), seizures (lowered threshold), anticholinergics (congestion, dry mouth,etc), phototoxicity, leukopenia (rare) |
|
|
Term
| antipsychotic neuro side effects |
|
Definition
| Involve involuntary motor activity in 1/3; Parkinsonian syndrome (block dopa), dystonias (treat w/ benztropine, diphenhydramine), akathisias (agitation, treat w/ anticholinergic benztropine), tardive dyskinesia (no treat, coordinated rhythmic involuntary tongue/mouth movements) |
|
|
Term
New "atypical" antipsychotics
Risperidone
clozapine
olanzapine
quetiapine
ziprasidone |
|
Definition
| fewer neuro side effects; as effective as halo on positive symptoms, better at negatives; blocks D2 and serotonin receptors; sever weight gain, type 2 diabetes |
|
|
Term
|
Definition
| Some prolactin elevation, causes neuro side effects at high doses |
|
|
Term
|
Definition
| very mild neuro side effects, no dyskinesia, no prolactinemia; get agranulocytosis; binds D4 10x higher than other dopa receptors, seen in mesolimbic system not in striatum |
|
|
Term
|
Definition
| Binds serotonin and D4 receptors, pretty high on D2; low incidence of neuro side effects, no prolactin increase |
|
|
Term
|
Definition
| high serotonin receptor affinity, some D2, antagonize H1 histamine (sedation) and alpha 1 (hypotension) receptors |
|
|
Term
|
Definition
| partial D2/5HT1A agonist and 5HY2A antagonist; little/no sedation, neuro side effects, hyperprolactin, hypotension |
|
|
Term
| Bipolar treatment with antipsychotics |
|
Definition
| aripiprazole, chlopromazine, olanzapine, quetiapine, risperidone, ziprasidone |
|
|
Term
|
Definition
| Low MW, infinitely soluble, can't be ionized, readily crosses membranes, absorbed in the duodenum |
|
|
Term
|
Definition
ethanol + NAD > acetaldehyde + NAD > acetic acid + CoA + ATP > acetyl CoA > TCA cycle CO2, H2O, calories; limiting factor = NAD
Minor path => ethanol + NADPH >CYP2E1 acetaldehyde |
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Term
|
Definition
| altered redox from increased NADPH, reduced NAD >fatty acid synth, decreased fat oxidation, free FA increase, triglycerides increase in liver |
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Term
|
Definition
GI=stim gastric acid secrete, increase ulcer likelihood, cause diarrhea
Cardio=vasodilation, sympathetic tone increased, increased cardiac output, tachycardia/arrythmias, increased HDL levels, reduce contractility |
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Term
|
Definition
| CNS depression, disinhibition, euphoria (increase in release of dopamine), activated reward pathways, drives further consumption |
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|
Term
| Ethanol effects peripherally |
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Definition
| vasopressin secretion inhibition (diuresis, dehydration, inhibit neurons of supraoptic/paraventricular nuclei); inhibit luteinizing hormone release (depress reproductive function |
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Term
|
Definition
| makes formaldehyde, causes metab acidosis, blindness and death; give alcohol, fomepizole |
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Term
|
Definition
| barbiturates and general anesthetics/other CNS depressants lower function, less tolerance of acute lethal effects |
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Term
|
Definition
| tremors, hyper-reflexia, sweating, muscle cramps, vomit, delirium tremens, visual halluc, hyperthermia, cardio collapse, tonic-clonic seizure |
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Term
|
Definition
| peripheral neuropathy, pellagra (vitamin defic), Wernicke's, Korsakoff's, Cerebellar degeneration |
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Term
|
Definition
| withdrawal=benzodiazepine, lorazepam, diazepam, carbamazepine |
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Term
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Definition
| antabuse, inhibit aldehyde dehydrogenase, accumulate acetaldehyde after ingestion, get vasodilation, nausea, vomit, syncope, misery; hepatitis, jaundice, fatigue, fever, ab pain |
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Term
|
Definition
| opiate antagonist, reduce reinforcing effects of alcohol |
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Term
|
Definition
| GABA analog, impair NMDA receptor function, reduce neuronal hyperexcitability, reduces cravings |
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Term
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Definition
| Sleep disturbances, loss of Interest, Guilt, decreased Energy and Concentration, Appetite changes, Psychomotor retard, Suicidal |
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|
Term
| Biogenic amine theory of depression |
|
Definition
| deficiency of serotonin or NE; most AD increase one/both |
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Term
| Neurogenesis theory of depression |
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Definition
| impaired hippocampal neurogenesis leads to depression, try to decrease cell death; depressed patients have smaller hippocampal volume |
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Term
MAOIs
tranylcypromine, phenelzine, selegiline |
|
Definition
| Block oxidative metab of biogenic amines, IRREVERSIBLY inhibit MAO-A&B; acute=CNS stimulation, agitation, euphoria; adv=orthostatic hypotension, CNS stimulation, GI distress, sexual dysfunction; OD uncommon, cause hyperthermia, shock, seizure; avoid indirect sympathomimics, tyramine, amphetamines, buproprion, L-DOPA, can cause hypertensive crisis; DON'T MIX WITH SSRI |
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Term
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Definition
| Rare but potentially fatal, ingestion of ecstasy and MAOIs; confusion, hypomania, hallucinations, agitation, headache, coma, shivering, sweating, hyperpyrexia, hypertension, tachycardia, nausea, diarrhea, twitches, hyperreflexia, tremor |
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Term
| Tricyclic antidepressants |
|
Definition
Tertiary=imipramine, amitriptyline; block serotonin reuptake, break down to secondary and block NE uptake
Secondary=desipramine, nortriptyline; block NE reuptake |
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Term
|
Definition
acute=drowsy, dysphoric, anxious, impaired cognition, autonomic effects; frequent toxicity, antagonize many different neurotrans receptors (histamine, ChMuscarinic);
Sedation, seizures, orthostatic hypotension, tachycardia, arrythmias, anticholinergic effects, increased appetite/weight gain; Low TI, coma, convulsions, cardiovascular in OD (arrythmia, seizure, acidosis, delirium, paralysis, coma); fast metab with neuroleptics, oral contraceptives, SSRI, slower with barbiturates, carbamazepine, rifampin; increase antiCh, sympathomimic, CNS depressant effects; block guanethidine and clonidine |
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|
Term
SSRIs
fluoxetine, sertraline, venlafaxine, duloxetine |
|
Definition
| Raise synaptic serotonin levels, more specific than TCAs, fewer side effects; Ven/Dulo inhibit 5-HT and NE uptake (SNRIs); don't block receptors; Fluox=high half life, little withdrawal issues |
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Term
|
Definition
| Acute=CNS stimulation, anxiety, agitation; not sedating, much safer in overdose; headache, GI upset, sexual dysfunction, insomnia, agitation, anxiety, increased blood pressure (rare); high TI, needs tapered off; Fluoxetine/Paroxetine inhibit P450 enzymes, avoid MAOIs (serotonin syndrome) |
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|
Term
|
Definition
| weak 5-HT and NE uptake, antagonize post synaptic 5-HT2A receptors; sedating, orthostatic hypoTN, nausea, dizzy from block alpha 1/H1/5-HT receptors; don't block muscarinic receptors |
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Term
|
Definition
| Inhibit 5-HT and NE uptake; dry mouth, nausea, agitation, insomnia (stimulant); treat nicotine addiction/withdrawal; OD=agitation, delirium, seizure |
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|
Term
|
Definition
| Antag presynaptic alpha 2 receptors, little effect on reuptake systems, antag 5-HT2/3 receptors; very potent H1 receptor antag (sedating, weight gain, inc appetite) |
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|
Term
| General antidepressant guideline |
|
Definition
| atypical=give MAOI; require 2-6 weeks for effect; SSRIs=1ST LINE FOR MOST; |
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Term
|
Definition
| deficiency in central monoamines leading to reduced ability to focus attention; stimulants alleviate the deficiency |
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Term
|
Definition
| Adderall, achieve steady blood levels of amphetamine; increased risk of heart attack, stroke, or sudden death |
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|
Term
|
Definition
| Ritalin; inhibits NE, DA, 5HT uptake, less reinforcing than cocaine; abuse less than amphetamines; crash unavoidable |
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|
Term
|
Definition
| NE selective reuptake inhibitor; not reinforcing, low abuse potential; drowsiness, sex dysfunction, inhib P450 2D6, suicidal thoughts |
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|
Term
| Acute manic episode of bipolar treatment |
|
Definition
| antipsychotics (olanzapine, quetiapine, aripiprazole), sedatives,antiseizure drugs (VALPROIC ACID, CARBAMAZEPINE, LAMOTRIGINE) |
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|
Term
|
Definition
| interferes with IP3 metab (2nd messengers), inhibits glycogen synthase kinase 3; long term bipolar maintenance; can't beat acute mania alone; very narrow TI; tremor, ataxia, hyperactivity, edema, mild hyopthyroid, polydipsia, polyuria, GI irritation; |
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|
Term
| Lithium OD and interactions |
|
Definition
| Acute=vomit, profuse diarrhea, coarse tremor, ataxia, seizure, come; moderate=above + confusion, aphasia, ataxia, hyperactivity, hypotension; supportive care for OD, give dialysis; absorbed well, short half-life, test blood levels to determine right dose; Inc lithium levels from sodium depleting diuretics (thiazides), NSAIDS increase toxicity chance; decreased Li levels due to increased excretion (mannitol, acetazolamide, theophylline) |
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|
Term
|
Definition
| May decrease sensitization of brain to repeated mood swings; valproate and carbamazepine used as adjuncts to lithium; quick response, CAN TREAT ACUTE MANIA; |
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Term
|
Definition
| Nociceptor neurons end in free endings, acts through A-gamma and C fibers; use substance P, arachidonic acid metabolites, prostaglandins, thromboxanes, leukotrienes |
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Term
|
Definition
| Myelinated A fibers and unmyelinated C fibers; spinothalamic pathway (rapid, discriminative pain); spinoreticular/mesencephalic path (slow, arousing pain) |
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Term
|
Definition
| Periaqueductal gray via raphe magnus to dorsal horn; descending activation reduces pain perception |
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|
Term
| methionine-enkephalin/leucine-enkephalin |
|
Definition
| distributed in brain, rapidly degraded by peptidases, regulate pain pathways via inhibition of pain nerves |
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|
Term
|
Definition
| found in brain (dorsalhorn), pituitary; rapidly degraded by peptidases |
|
|
Term
|
Definition
| co-synthesized with ACTH or alpha MSH; found in hypothalamus, brain stem, pituitary; relatively stable |
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|
Term
| Transcutaneous electrical nerve stimulation |
|
Definition
| enhances descending pain control over ascending pain signal |
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Term
|
Definition
| Significant first pass metabolism, all but oral are good routes; distribute to all tissues, mostly in parenchymal organs; aromatic ring with group at position 3 (-OH most potent); major metab via conjugation w/glucuronic acid, makes morphine more potent; minor metab via N-demethylation; excreted in urine and bile |
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|
Term
|
Definition
| mu=mediates analgesia, anesthesia, sedation, miosis, euphoria, constipation, resp depression, OPIATE DRUGS ACT ON IT, tolerance/dependence; kappa=analgesia, miosis, sedation, DYSPHORIA; delta=influence affective behavior |
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Term
|
Definition
| opiod partial agonist, morphine-like action with lower maximal effect for mild pain |
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Term
|
Definition
| opiod antagonists, treat acute opiate overdose; nalox must be injected, naltrex oral OK and longer duration, treats opiod addiction |
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|
Term
| Opiod receptor activation |
|
Definition
| increased K conductance (hyperpol), reduced Ca conductance (diminished transmitter release), inhibition of adenylyl cyclase (short term, inhibit transmitter release) |
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|
Term
|
Definition
| 10 mg for moderate; 15-20 for severe, causes N/V, drowsiness, resp depression; not effect touch, temp, sight, and sound |
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|
Term
|
Definition
| Dorsal horn of cord, raphe magnus, periaqueductal gray, thalamus; relief 2-5 hours, lead to tolerance/dependence |
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|
Term
|
Definition
| cough suppressant, elevate cough threshold |
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|
Term
|
Definition
| centrally suppress coughing, NO effect on opiod receptors, act as NMDA receptor antagonist |
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|
Term
|
Definition
| super potent opiod, anesthetic, transdermal application; severe resp depress at high dose, require muscle relaxant for surgery; no peripheral vasodilate (good for cardiac surgery), rapidly reversed w/ antagonist; needs NO2 to fully knock out |
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|
Term
| Morphine effect on cardiovascular |
|
Definition
| treats MI pain, may exert cardioprotective effect by opening K channels |
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|
Term
|
Definition
| euphoria, sedation, reduced anxiety; act on mu receptor in VTA and nucleus accumbens |
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Term
|
Definition
| Constipation, reduced gut motility, increased water retention, increased sphincter tone, constriction of the bile duct |
|
|
Term
|
Definition
| Increase prolactin, growth hormone; reduced TSH, ACTH, LH; reduced sexual drive, sperm motility, ejaculate volume |
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Term
|
Definition
| more potent than morphine, lasts 3-5 hours |
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|
Term
|
Definition
| equal potency as morphine, orally active, analgesic and heroin addiction therapy |
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|
Term
|
Definition
| less potent/shorter thand morphine |
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|
Term
|
Definition
| weaker drug (like codeine), analgesic for mild pain |
|
|
Term
|
Definition
| highly potent meperidine analog, controls diarrhea, won't enter brain, no abuse |
|
|
Term
|
Definition
Nalo=treat overdose, short duration
Naltrex=long antaganist, treat opiate addiction |
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|
Term
|
Definition
|
|
Term
|
Definition
| isomer of active opiate, little or no effect on opiate receptors; act as antagonist on NMDA receptors in medulla; cough suppressant in OTC preps |
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|
Term
|
Definition
| Increase activity of DA neurons in VTA, sends axons to nucleus accumbens/prefrontal cortex/forebrain; Substantia nigra sends to caudate and putamen |
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|
Term
| Dopamine pathway functions |
|
Definition
VTA->NAc=reward, behavior reinforcement
VTA->PFC=cognitive reward, learning
SN->CPu=habit learning, compulsive behavior |
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Term
|
Definition
| regulated by glutamate, GABA, endogenous opiods/cannabinoids, and other neurotransmitters |
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|
Term
|
Definition
| blocks adenosine-R through GPCR |
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|
Term
|
Definition
| Targets serotonin receptor, acts through GPCR, increases IP3, causes depolarization |
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|
Term
|
Definition
| acts through nACHn-R, increases cation conductance |
|
|
Term
|
Definition
| GABA-A receptor target, potentiates GABA through ion channels, leads to hyperpolarization and sedation |
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|
Term
|
Definition
| Blocks NMDA-R, inhibits glutamate; leads to hallucination and disorientation |
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|
Term
|
Definition
| displaces DA, increases DA in synapses |
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|
Term
|
Definition
| displaces serotonin; increase serotonin in synapse |
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|
Term
| Opiate withdrawal symptoms |
|
Definition
Early (6-12 hrs)=tears, runny nose, yawning, sweating, anxiety;
16-96 hrs=mydriasis, anorexia, goosebumps, restlessness, irritability, tremor, weakness, depression, N/V, intestinal spasms, diarrhea, muscle/back pain, spasms, CNS stimulation, weight loss, acid-base change, dehydration, ketosis; opposite of acute toxicity |
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|
Term
|
Definition
| centrally active adrenergic alpha 2 agonist, reduces severity of opiate withdrawal, reduces activity of noradrenergic neurons in locus ceruleus |
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|
Term
|
Definition
| increase HR/BP; short duration IV/smoke, longer orally; blocks NA/DA/5-HT re-uptake; high doses=enlarged heart, psychosis, paranoia; withdrawal=increased appetite, lethargy, chronic depression, sexual dysfunction |
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|
Term
|
Definition
| resembles both endogenous catecholamines and sympathetomimetic decongestant drugs; CNS stimulation, increase alertness/concentration/delayed fatigue, elation, euphoria, irritability, anxiety |
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|
Term
|
Definition
| indirectly acting, release NE/DA/5-HT from terminals; meth>d>l enters brain easier, longer half life; enters neurons by diffusion/DA transporter/NE transporter; inhibits MAO; sever paranoia/psychosis, arrythmias, paroxysmal tachycardia, heart block, extreme addiction, dental issues; relapse high, chronic brain damage |
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|
Term
|
Definition
Acute overdose=agitation and seizure control w/ diazepam;
Addiction=irritability/lethargy/hunger, ahedonia, NO TREATMENT |
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Term
|
Definition
| anti-emetic synthetic analogues of THC |
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|
Term
|
Definition
| rapid absorption after smoking, peak at 10-30 minutes, redistribute to adipose quickly, metab in liver, excreted in urine/feces in 5 days, urine detectable for 24 hrs |
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|
Term
|
Definition
| Tachycardia, euphoria, visual/auditory/temporal distortion, relaxation/sedation, psychomotor impairment, dry mouth, hunger, peripheral vasodilation; high dose=very confused, disorganized thinking, hallucinations, delusions, anxiety, panic, paranoia |
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|
Term
|
Definition
| CB1 receptors in CNS, CB2 in periphery; inhibit adenylyl cyclase; CB1 in hippocampus/cortex/striatum/NA, influence memory, cognition, motor function, and reinforcement |
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|
Term
|
Definition
| CB1 antagonist, approved for weight loss in obese, increase depression and suicide; reduces relapse in abstaining chronic tobacco smokers |
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|
Term
|
Definition
| endogenous lipid w/ high affinity for CB receptors; used in extinction of learned memories (mostly fearful memories); functional regulator of some immune responses |
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|
Term
|
Definition
| chemo-induced vomiting, reduce glaucoma pressure, pain relief (potentiate other analgesics) |
|
|
Term
| Chronic marijuana use problems |
|
Definition
| bronchitis, asthma (higher carcinogen concentration than cigarettes), suppression of the immune response, decreased sex steroid secretion, amotivational syndrome, severe memory loss; slow tolerance |
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|
Term
|
Definition
| very potent, last 12 hrs; dizziness, dilation, weakness, tremor, nausea, paresthesia, blurred vision, difficulty focusing, altered awareness, elation, euphoria/dysphoria, depression, fear, paranoia, panic; detachment after 6 hrs; PARTIAL AGONIST AT 5HT2 receptors; marked tolerance |
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|
Term
|
Definition
| analgesia, amnesia, poor muscle relaxation, 40% dysphoric rxns, violent psychosis; non-competitive NMDA receptor antagonis; mimics intoxication; blank stare, catatonia, confusion, drowsiness, HYPERSALIVATION, sweating; high doses=stupor/coma 4-6hrs, paranoid psychosis; chronic=persistent difficulty thinking, memory deficits, speech impairment |
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Term
|
Definition
| Symptomatic only, no direct treatment |
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Term
|
Definition
| mast cells, eosinophils, T-lymphocytes, macrophages, neutrophils, epithelial cells, smooth muscle cells |
|
|
Term
|
Definition
Extrinsic (allergic)-increased serum IgE
Intrinsic -pathophys disturbances, negative response to common antigenic challenge |
|
|
Term
| Early/immediate symptoms of IgE asthma |
|
Definition
| bronchoconstriction/vascular leak, histamine, proteases, leukotrienes C4 & D4, prostaglandins |
|
|
Term
| Late/sustained symptoms of IgE asthma |
|
Definition
| bronchoconstriction, cellular infiltration, mucus hypersecretion, Th2 cytokines (IL-3,4,5,9,13) |
|
|
Term
| Nonspecific bronchial hyperactivity |
|
Definition
| Caused by viral upper respiratory infection, exercise/rapid respiratory maneuvers, cold air, chemicals; caused by inflammation of the airway |
|
|
Term
| Stages of airway inflammation |
|
Definition
Acute-early recruitment of cells
Sub-acute-cells activated to cause a more persistent pattern of inflammation
Chronic-persistent level of cell damage and an ongoing repair process, may cause permanent abnormalities in airway |
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|
Term
|
Definition
| Beta-adrenergic agonists, muscarinic antagonists, methylxanthines; increase smooth muscle relaxation or decrease smooth muscle contraction |
|
|
Term
|
Definition
| corticosteroids, leukotriene pathway modifiers, release inhibitors, anti-IgE therapy |
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|
Term
Beta-2 adrenergic receptor agonist
Albuterol |
|
Definition
| RESCUE MEDICATION; regular use may potentiate bronchial hyperresponsiveness; relaxes smooth muscle in airway, inhibits mast cell release of bronchoconstrictors, inhibits microvascular leakage, increase mucociliary transport, stimulate adenylyl cyclase |
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|
Term
| Long acting beta agonists |
|
Definition
| salmeterol, formoterol; very selective, slow onset, used for maintenance; in combination with corticosteroids=better results for persistent asthma |
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|
Term
Muscarinic antagonists
Tiotropium |
|
Definition
Slightly less affective than beta agonists in reversing bronchospasm, used if intolerant of B-agonist; systemic adverse effects; enhanced by albuterol in acute attacks; blocks acetylcholine=blocks bronchoconstriction and secretion of mucus;
Tiotropium=long M1 & M3 acting |
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|
Term
Methylxanthines
Theophylline |
|
Definition
| Lowest cost and high compliance; relaxes smooth muscle, stimulates CNS/cardiac muscle, diuretic; ANTAGONIZE ADENOSINE RECEPTORS, INHIBITS PHOSPHODIESTERASE=>elevated cAMP; affects intracellular calcium concentration; readily absorbed, causes arousal, tremor, convulsions, tachycardia, arrythmias, weak diureti, MANY DRUG INTERACTIONS, especially with macrolide antibiotics, narrow therapeutic index |
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|
Term
Corticosteroids
fluticasone |
|
Definition
Most potent anti-inflammatory medication currently available; FIRST LINE FOR LONG TERM CONTROL of asthma; reduce bronchial reactivity; act through glucocorticoid receptors to regulate gene expression, inhibit eosinophil induced inflammation/cytokine production/phospholipase A2 activity, decreased prostaglandin/leukotriene synthesis;
Inhaled=few effects (cataracts, decreased bone density, oral candida), oral=severe effects (weight gain, bone loss, Cushing's, adrenal suppression) |
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|
Term
Leukotriene receptor antagonists/synthesis inhibitors
Montelukast |
|
Definition
Alternatives/adjuncts to inhaled corticosteroids; good for aspirin/exercise induced asthma, oral/long lasting/less effective than steroids; NOT A RESCUE MED;
Montelukast=CysLT1 receptor antagonist, lasts 24 hrs |
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|
Term
|
Definition
| Prophylaxis onle, no effect on airway smooth muscletone, never first line; used regularly can reduce bronchial hyperactivity; minor side effects in throat; inhibit delayed chloride channels=>reduced accumulation of calcium in mast cells=>decreased mast cell degranulation, inhibit IgE production by B lymphos |
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|
Term
|
Definition
| anti-IgE antibody; removes circulating IgE, injected every 2-4 weeks; potential anaphylaxis, used only in severe patients |
|
|
Term
|
Definition
Progressive, not inflammation driven, remodels the lung parenchyma, higher risk of infection and air trapping;
Albuterol=reduced resistance/bronchospasm
Tiotropium=reduce spasm
Fluticasone=only use with albut/tiotrop |
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|
Term
|
Definition
| biologically active locally acting substances that are not steroids |
|
|
Term
|
Definition
| Neurotransmitter in PNS/CNS, mediates vasodilation, can kill/inhibit growth of target cells in high doses; made by NO synthase |
|
|
Term
endothelial NOS
neuronal NOS
inducible NOS |
|
Definition
eNOS/nNOS=constitutively expressed, activated by calcium/calmodulin binding, activated by stimuli that increases intracellular calium levels
iNOS=induced after stimulation of cells with cytokines/microbes.microbial products; constitutively active once expressed, produces large amounts NO |
|
|
Term
Prostaglandins
Misoprostol |
|
Definition
| eicosanoids from the arachidonic acid, synthesized as a response, act through G-proteins; potent vasodilate, cause hypotension/headache/flushing; inhibit gastric acid secretion; contract uterine smooth muscle, |
|
|
Term
Alprostadil
Misoprostol
Iloprost |
|
Definition
PGE-1 analogue, helps erectile dysfxn
PGE-1, helps gastric ulcers/cause abortion
Prostacyclin, Raynaud's & primary arterial HTN |
|
|
Term
|
Definition
| erection from smooth muscle relaxation, need parasympathetic signal and NO via cAMP/cGMP increase |
|
|
Term
|
Definition
| cGMP phosphodiesterase inhibitor=> cGMP increase; short half life (4-5 hours); NEVER TAKE WITH NITRATES (too much vasodilation), slight visual dysfunction (cGMP-ase in retina), headache, flushing, dyspepsia, nasal congestion |
|
|
Term
|
Definition
| local, 15 second half life, PAIN CAUSING, potent vasodilation/vascular permeability, prostaglandin/autocoid synthesis, acts thru B1/B2 receptors (B1=upregulated in inflam, B2 constitutive, release NO) |
|
|
Term
|
Definition
CNS, PNS, enteric NS arteriolar relaxant; acts thru tachykinin receptors;
P receptor antagonist used as antiemetic |
|
|
Term
| Calcitonin gene related peptide |
|
Definition
| derived from calcitonin gene, CNS/PNS/enteric NS, cardio/uro systems; most potent vasodilator known, may cause migraines |
|
|
Term
|
Definition
stored in inert form, highest in lung/skin/stomach/gut in mast cells/basophils/CNS/gut mucosa;
Neg reg own release through H2 on mast cells |
|
|
Term
|
Definition
| Degranulation releases histamine/prostaglandins/ATP/leukotrienes causing inflam/local vasodilate |
|
|
Term
| Histamine release via chemical/cellular injury |
|
Definition
unexpected anaphylaxis thru specific increase in intracellular Ca2+;
cytolytic release when plasma membrane is damaged |
|
|
Term
|
Definition
smooth mm, endothelium, brain; IP3/Ca2+ incr.
gastric mucosa, cardiac mm, mast cells; cAMP incr.
Presynaptic CNS/PNS/myenteric plexus; Ca2+ incr, cAMP inhibit
GI tract; Ca2+ incr, cAMP inhibit |
|
|
Term
Histamine action:
Cardio
Smooth mm
Sensory
Secretory
Skin
CNS |
|
Definition
vasodilation, increased capillary permeability,decrease systemic BP;
Contraction, increased motility and bronchocontriction(H1)
Pain and itching (H1)
Gastric acid secretion (H2)
Wheal and Flare (H1)
Cardio/neuroendocrine/thermoreg/arousal control (H1,2,3), wakefulness in hypothalamus (H1) |
|
|
Term
|
Definition
1st generation= small molecules, cross BBB, cross-react, OTC, cause sedation
2nd generation= larger lipophilics, more specific to H1, prescription only, non-sedating |
|
|
Term
| 1st generation antihistamine |
|
Definition
dimenhydrinate
diphenhydramine (antitussive, too)
meclizine
promethazine
treat N/V, vertigo |
|
|
Term
| 2nd generation antihistamines |
|
Definition
|
|
Term
|
Definition
| treat nasal allergies, ancillary treatment of anaphylaxis, sedatives (1st gen) with tolerance; |
|
|
Term
|
Definition
| most via CYP450s, half lives prolonged in elderly, children hypermetabolize |
|
|
Term
| Antihistamine adverse rxns |
|
Definition
1st gen=sedation, dizzy, low alertness, slow rxn time, reduced visual acuity, impaired cognition, anticholinergic effects (dry mouth, poor urinatino, ED), loss/gain appetite, nausea, GI distress
2nd gen=no adverse effects |
|
|
Term
|
Definition
secreted by carcinoid tumors; stimulate intestinal smooth mm, diarrhea, ab pain;
5-HT1D/5-HT1F receptor ligand, treat migraine |
|
|
Term
|
Definition
| activate meningeal/blood vessel nociceptors and alter central pain modulation; trigeminal sensory neurons release CGRP/neurokinin A/substance P inducing vasodilation/extravasation/hyperalgesia |
|
|
Term
|
Definition
| Migraine treat; 5-HT1 agonist, activate inhibatory 5-HT1D receptors, prevent nociceptor impulses; little cross rxn (reduce side effects); constrict coronary vessels (CONTRA angina/ischemic heart disease); CONTRA MAOI (may build up sumatriptan) |
|
|
Term
Ergotamine
dihydroergotamine |
|
Definition
| Migraine treat; Interact with alpha-adrenergic/dopamine/serotonin receptors; adverse=periph vasoconstriction, diarrhea, nausea, vomit; CONTRA pregnant, coronary HD, impaired liver fxn |
|
|
Term
|
Definition
beta blockers (propranolol)
ergot alkaloids (methysergide)
antidepressants (amitriptyline)
calcium channel blockers (verapamil)
antiseizures (valproate/topiramate/gabapentin)
NSAIDS (ibuprofen) |
|
|
Term
|
Definition
| Macros etc release lysosomal enzymes/NO/hydrogen peroxide/radicals and disrupt cell membranes; released phospholipids convert to arachidonic, converts to leukotrienes by COX, converts to leuko/prosta/thombox and exacerbate inflam |
|
|
Term
|
Definition
| constitutive in most tissues, generally protective as vasodilator; fix peripheral resistance and kidney flow, blood clotting, uterine contract, muscle growth, CNS synaptic transmission |
|
|
Term
|
Definition
| Inducible; inflammation, wound healing; generate unstable endoperoxide intermediate |
|
|
Term
|
Definition
| induces expression of cytokines (IL-1,6), IFN beta, cell adhesion molecules |
|
|
Term
| Disease modifying anti-rheumatic drugs |
|
Definition
| gold, low dose steroids,etc. No analgesic/anti-inflam effect but reduce symptoms slowly/delay disease process |
|
|
Term
|
Definition
| most widely used DMARD, oral dose weekly works in 4-6 weeks; adv=anorexia, vomit, ab cramp, increased liver enzyme, immuno/marrow suppress, lymphomas |
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Term
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Definition
| retard bone/articular destruction by depressing macrophage fxn after ingestion by cells; adv=dermatitis, thrombocytopenia, aplastic anemia, proteinuria |
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Term
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Definition
| oral, immunosuppressant, inhibits dihydroorotate dehydrogenase (impaired lympho prolif); slows joint destruction |
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Term
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Definition
| TNF-alpha antagonist; prevents stimulation of receptors on immunoglobulin; inject 2x week |
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Term
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Definition
| TNF-alpha chimeric monoclonal Ab, binds free TNF-a, reduces joint swelling/damage via IV |
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Term
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Definition
| Reduces TNF-a production, modulates co-stim signal required for full T-cell activation |
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Term
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Definition
| chimeric anti-CD20 monoclonal antibody, depletes CD20 B cells |
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Term
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Definition
| IRREVERSIBLE non-selective COX inhibitor by acetylating the enzyme |
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Term
Older NSAIDs
ibuprofen, naproxen |
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Definition
| reversible non-selective COX inhibitors, cause gastric ulceration and impaired kidney fxn |
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Term
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Definition
| COX-2 selective NSAID, rediced GI damage, platelet aggregation not impaired; does cause impaired cardio fxn |
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Term
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Definition
| analgesic/antipyretic, less effective as anti-inflam, weak COX-1/2 inhib |
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Term
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Definition
| inhibit arachidonic production, inhibit COX-2, inhibit NF-kB |
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Term
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Definition
| Take other NSAID right after or long before aspirin to competitively inhibit COX-1 reversibly before aspirin can kill it; limits anti-platelet actions |
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Term
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Definition
| hyperplasia of renal juxtaglomerular apparatus, hyperreninemia, hyperaldosteronism, hypokalemic alkalosis, normal BP, PG excretion increased; NSAIDS REVERSE SYMPTOMS |
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Term
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Definition
| NSAIDs allow duct to close without surgery |
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Term
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Definition
Liver; short half life=aspirin, ibuprofen, indomethacin
long half life=naproxen, salicylate
MOST NSAIDs HIGHLY BOUND TO ALBUMIN |
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Term
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Definition
| convert to NAPQ1=hepatotoxin; impairs Ca2+ handling, causes necrosis |
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Term
| Renal adverse NSAID effects |
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Definition
| COX 2 required for normal development, probably in normal fxn too. NSAID abuse=reduced glomer filtration, edema, papillary necrosis, acute/chronic renal failure, interstitial nephritis, hyperkalemia |
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Term
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Definition
| develop bronchospams and resp failure by shunting arachidonic metabolism from COX path to leukotriene path |
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Term
| COX inhibitor side effects/contras |
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Definition
Skin=erythema multiforme, urticaria
CNS=drowsiness, headache
Rare=blood dyscrasias, liver dysfxn,neuro
CONTRA=pregnancy, hypersensitivities to NSAIDs, bleeding abnormalities |
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Term
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Definition
Reye's syndrome in flu/varicella infxn
nausea, vomit, tinnitus, GI bleed, hemostasis, respiratory alkalosis (low dose), resp/metab acidosis (high dose) |
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Term
| NSAID/COX inhibitor interactions |
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Definition
| drugs bound to plasma proteins, increased GI bleed after alcohol, lithium impaired clearance, potassium sparing diuretics cause hyperkalemia |
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Term
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Definition
| Promote duodenal ulcer healing, increase LES pressure, BAD with peptic ulcers |
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Term
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Definition
| High neutralization, lower gastric motility; osteoporosis in renal insufficients |
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Term
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Definition
| High neutralization, increased gastric motility; hypermagnesmia in renal insufficients |
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Term
|
Definition
| Moderate neutralization, causes milk-alkali syndrome, hypercalcemia, bloating |
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Term
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Definition
| High neutralization, causes systemic alkalosis, bloating |
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Term
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Definition
| mucosal protective agent, physically protects and makes a viscous layer over ulcers; NEEDS EMPTY STOMACH |
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Term
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Definition
| Pepto, mucosal protectant; binds ulcer site, bind bile acid, stimulates prostaglandin and alkali secretion; IF ALLERGIC TO ASPIRIN, AVOID THIS! |
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Term
H2 receptor antagonists
Cimetidine, ranitidine |
|
Definition
| structural analogs of histamine, competitive inhibition of H2 on gastric parietal cells; limited CNS if at all; inhibit gastrin stimulated/muscarinic acid secretion; rapid absorption and very short half life |
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Term
| Cimetidine toxicity/interact |
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Definition
| gynecomastia, galactorrhea, headache, fatigue, GI disturbances; interacts with P450, prolongs phenobarbital, theophylline, diazepam, etc |
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Term
Proton pump inhibitors
Omeprazole, esomeptazole, rabeprazole |
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Definition
| short term duodenal/gastric ulcers, GERD, Zollinger-Ellison, eradicates H.Pylori; IRREVERSIBLE INHIBIT proton pump by 90%, activated at low pH; gets absorbed, pumped into canaliculi, turn around and kill pump. PUMP MUST BE ON TO CAUSE RELEASE AND INDUCE BINDING; well tolerated, only nausea, diarrhea, ab pain, constipation assoc., increased risk resp infxn/pneumo in prolonged use, INCREASED HIP FRACTURES; reduce absorption of drugs needing low pH |
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Term
Prostaglandins
misoprostol |
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Definition
| prostaglandin E1 analog, inhibits gastric acid secretion, stimulates mucin secretion; cause diarrhea, potential abortion; NEVER USE IN PREGNANCY |
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Term
|
Definition
Quadruple drug=PPI/H2RA, metronidazole, tetracyclin, pepto
Triple=PPI, clarithromycin, metronidazole |
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Term
Prokinetic agents
Metaclopramide |
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Definition
| stimulate emptying by cholinergic input, ihibited by adrenergic input; Stimulated by D2 receptor antag, 5-HT3 antag, 5-HT4 AGONIST (Meto action) |
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Term
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Definition
| 5-HT3 receptor antagonist/5-HT4 agonist; stimulate ACh release from myenteric neurons, increase cholinergic input, RASIE LES pressure, INCREASE emptying, DECREASE small bowel transit time; freely enters CNS (anti-emetic); PARKINSONISM from dopamine agonism, TARDIVE DYSKINESIA |
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Term
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Definition
| Treat IBS/peptic ulcer; bad side effects |
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Term
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Definition
| regulated by lateral reticular formation of medulla/chemoreceptor trigger zone of area postrema (no BBB, gets signals from blood) |
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Term
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Definition
Serotonin on 5-HT3 receptors
Dopamine on D2 receptors
ACh through M1 (motion sickness)
Histamine on H1
Delayed gastric emptying |
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Term
D2 receptor antagonists
Metoclopramide
Droperidol |
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Definition
Inhibit D2 receptors at CTZ, induce hypotension
Drop=post-op N/V prophylaxis; cause hypotension, drowsiness, dysphoria, arrhythmias |
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Term
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Definition
| 5-HT3 receptor antagonists exclusively , no extrapyramidal side effects, effective in radiotherapy emesis; mild headache, constipation, diarrhea, dizzy |
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Term
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Definition
| Substance P (Neurokinin-1) receptor antagonist, help chemo-induced therapy/post-op nausea/vomit |
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Term
|
Definition
| H1 antihistamine, battle motion sickness |
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Term
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Definition
| Cannabinoid, act at central CB1 receptors, treat chemo-emesis |
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Term
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Definition
| Non-aspirin 5-aminosalicylates for IBS; act by inhibition of arachidonic production in colon |
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Term
|
Definition
| Antidiarrheal opiod agonists, inhibit ACh release in enteric nervous system, reduce motility; CNS penetration poor |
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Term
|
Definition
| Treat diarrheal IBS, antagonize 5-HT3 in women |
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Term
|
Definition
| 5-HT4 agonist for constipation IBS in women/idiopathic chronic constipation in all; side effects=diarrhea, flatulence, cholecystitis; SERIOUS MI/STROKE RISK |
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Term
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Definition
| metabolite of PGE1, opens chloride channel ClC-2; increases intestinal water secretion; adv=delayed gastric emptying |
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Term
|
Definition
| opioid antagonists peripherally at mu-receptors, no BBB cross, don't interfere w/ pain drugs; ONLY FOR POST-OP ILEUS |
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Term
| Sodium phosphate/bisphosphate |
|
Definition
| oral osmotically active agent to promote water retention in distal ileum/colon, CONTRA IN RENAL DAMAGED |
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Term
|
Definition
| osmotically active laxative |
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Term
|
Definition
| Stimulant laxatives, promote accumulation of water/electrolytes in lumen, stimulate motility; potent and quick |
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