Pharm Ch 13 (Chronic Neurologic Disorders)

this primarily involves a loss of dopamine signaling but can also involve acetylcholine
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Terms in this set (117)
this primarily involves a loss of dopamine signaling but can also involve acetylcholine
parkinson's disease
this involves overactive neuronal activation
seizure disorders
current treatment for this involves increasing acetylcholine levels
Alzheimer's disease
this is activated under non-stressful conditions, rest and digest, digestive process is promotes, heart rate and blood pressure decline, primarily modulated by acetylcholine
parasympathetic nervous system
this is activated under stress, fight or flight, readies the body for an immediate response to a potential threat, and is mostly modulated by norepinephrine and epinephrine
sympathetic nervous system
the receptors located at parasympathetic target sites
muscarinic receptors
effects of this system are cholinergic effects (pupil constricts, stimulates salivation, slow heart rate, constrict bronchioles, stimulate digestion, stimulate gallbladder function, contract bladder, stimulates erection and vaginal lubrication)
parasympathetic
effects of this system are anticholinergic (dilate pupil, inhibit salivation, inc heart rate, dilate bronchioles, inhibits digestion, stimulates release of glucose, secretes epi and norepi, relaxes bladder, and stimulates ejaculation and orgasm
sympathetic
with a drug that blocks acetylcholinesterase, what will happen?
increase in parasympathetic responses
prototype drug for cholinesterase inhibitors
neostigmine
this drug inhibits acetylcholinesterase which reverses toxic and life-threatening delirium caused by anticholinergic agentsneostigminethe use for this drug is for reversing life threatening delirium, glaucoma, Alzheimer's, and myasthenia gravisneostigmineadverse effects of this drug are excessive muscarinic stimulation (increased GI motility, increased salivation, bradycardia, urinary urgency, twitching)neostigmineadverse effects of this drug can lead to CHOLINERGIC CRISISneostigminethis drug is first line therapy for Alzheimer's and is used for cognitive dysfunction in late-stage Parkinson's diseasedonepezilthis drug is for temporary improvement or stabilization of dementia, and is a cholinesterase inhibitordonepeziladverse effects of this drug are usually a result of excessive muscarinic stimulation (excessive salivation, diarrhea, bradycardia, urinary urgency)donepezilwith this adverse effect of cholinesterase inhibitors, patients will experience respiratory depressioncholinergic crisisHow to reverse cholinergic crisis (antidote for all cholinesterase inhibitors)atropine (anticholinergic) to raise HRthis is caused by the destruction of the substantia nigra which is part of the basal gangliaparkinsonismL-dopa cancross the BBB!!!Once L-dopa converts to dopamine itcan't cross the BBB_______ prevents conversion of L-dopa peripherallycarbidopaprototype for COMT inhibitorsentacapone and tolcaponethese slow conversion of L-dopa to dopamine so more L-dopa crosses the BBBCOMT inhibitorsDopamine is metabolized bymonoamine oxidasethese keep dopamine available in the CNS longerMAO-B inhibitorsdopamine synthesis drugslevodopa/carbidopadopamine agonist drugspramipexole, bromocriptine, ropinirole, apomorphinedopamine releaser drugamantadinecatecholamine-o-methyltransferase (COMT) inhibitorsentacapone, tolcaponemonoamine oxidase-b (MAO-B) inhibitorsselegiline, rasagilineThis drug crosses the BBB, whereas dopamine alone cannot. It is taken up by dopaminergic nerve terminals and converted to dopamine. This newly-synthesized DA is released into the synaptic space and causes stimulation of DA receptors this restoring a proper balance between dopamine and acetylcholinelevodopathis drug is used to augment levodopa by decreasing the amount of levodopa that is converted to DA in the intestine and periphery. This results in larger amounts of levodopa reaching the CNScarbidopatwo enzymes that also break down dopamine and/or levodopa called _______ and _______COMT, MAO-Bthis drug inhibits COMT in periphery to prevent breakdown of levodopaentacaponethese drugs block MAO-B in the brain to selectively prevent breakdown of dopamineselegiline and rasagilinethese are direct agonists at dopamine receptorsparmipexole, ropinirole, and apomorphinethis drug increases dopamine release and blocks reuptakeamantadineprimary use for these drugs are to increase the levels of dopamine in the brain to relieve symptoms of Parkinson's disease, most effective treatment for PD but benefits wear off by year 5levodopa/carbidopaadverse effects of these drugs are N/V, drowsiness, dyskinesias, orthostatic hypotension, tachycardia and palpitations, psychosis, discoloration of sweat and urine, hallucinations, nightmares, activation of malignant melanomaslevodopa/carbidopawhen taking levodopa/carbidopa, avoid foods with _______ which can reduce the therapeutic effectspyridoxine (wheat, green veggies, bananas, whole grain cereals)this drug is considered a "rescue" medication for relief when symptoms are bad, and is given Subq like an Epi penapomorphinethese drugs activate dopamine receptors (agonists)pramipexole, ropinirole, apomorphineadverse effects of these drugs are nausea, sudden inability to stay awake, daytime sleepiness, orthostatic hypotension, psychosis, impulse control disorder, dyskinesiaspramipexole, ropinirole, apomorphinethis drug releases dopamine from the neuron and prevents dopamine reuptake, it also blocks cholinergic and glutamate receptorsamantadinedopamine releaseramantadineadverse effects of this drug is CNS effects, anticholinergic effects, discoloration of the skin (livedo reticularis)amantadinecommon pre-op medicineatropinetolcapone takes atoll on your liverthis drug blocks the enzyme COMTentacaponethis drug inhibits the metabolism of l-dopa in the intestines and peripheral tissues (and in the brain) so more l-dopa can move into the brain and remain thereentacaponeadverse effects of this drug are GI issues, discoloration of urine to a yellow-orage, rhabdomyolysis (muscle pain, tendon weakness), and liver failureentacapone and tolcaponemonitor liver function with these drugsCOMT inibitorsthese drugs block the enzyme MAO-B which is specific for dopamine metabolism in the brain. this leaves more dopamine in the brainselegiline, rasagilineuse for these drugs are to inhibit the metabolism of dopamine in the brain to offset the "wear off" effect of levo/carbi therapy and increases the window of l-dopa for up to 2 yearsselegiline, rasagilineadverse effects of these meds are insomnia (take before noon!), hypertensive crisisselegiline and rasagilinethis drug is converted to amphetamine so it should not be administered later than noon to prevent insomnia as an adverse effectselegilineavoid taking these medication with MAO-B inhibitorsMAOIs and antidepressantsthese drugs are antagonists at muscarinic acetylcholine receptorsbenztropine, trihexyphenidylthese drugs are centrally-acting anticholinergicsbenztropine and trihexyphenidylthese drugs diminish the excess cholinergic effect that may occur with loss of dopamine signaling as Parkinson's disease advancesbenztropine, trihexyphenidyladverse effects of these drugs are nausea, diarrhea, anticholinergic effects, antihistamine effects (sedation, drowsiness, confusion)benztropine, trihexyphenidylwhen parkinson's meds are at peak levels, ______ may be more commondyskinesiasmeds for this are best absorbed on an empty stomachparkinson's diseasefor people taking meds for PD, what should they avoid?high protein meals and snacksgoal of antiepileptic drugsreduce frequency and severity of seizuresall seizure drugs have ______ warningspregnancythis drug is given IV for status epilepticus (continuous seizure!!!)lorazepamprototype for traditional antiepileptics barbituratesphenobarbital, primidonethese drugs enhance inhibitory GABA receptor activityphenobarbital, primidonethese drugs are used for CNS depression to reduce neuronal activity, for simple partial, complex partial, secondary generalized, and tonic clonic seizuresphenobarbital, primidoneadverse effects of these drugs are CNS effects, toxicity (nystagmus, ataxia, resp depression), decreases synthesis of vit K and D, and decreases effectiveness of warfarinphenobarbital, primidonethree benzos you can give parenterallymidazolam, diazepam, lorazepamnever administer two ________ togetherbarbituratessymptoms of toxicity of this type of drug are nystagmus, ataxia, resp depress, coma, pinpoint pupils, hypotensionbarbituratesprototype trad. antiepileptics hydantoinsphenytointhis drug blocks voltage-gated sodium channels, slowing conduction and preventing high frequency firingphenytointhe use for this drug is to decrease seizure activity and prevent propagation of seizure activity, for all except absence seizures, and prevents seizures after brain surgeryphenytoincompared to barbiturates, this drug has less CNS depression and no potential for abuse/dependencyphenytoinadverse effects of this drug are CNS effects, gingival hyperplasia (gum issues), skin rash, cardio effects, endocrine effects (hirsutism), interference with vit K clotting can cause bleeding in newbornsphenytoinphenytoin has lots ofdrug-drug interactionsPhenytoin can only be given or diluted withSALINE (lots and lots of interactions)this med is very toxic to soft tissues, you should avoid hand veins when giving (purple glove syndrome), nd should give in a large central vein when possiblephenytointhis drug blocks voltage-gated sodium channels, prevents repetitive and sustained firing and may also increase serotonin activitycarbamazepinethis drug is used to decrease seizure activity and prevent propagation of seizure activity, helps with simple partial, complex partial, secondary general, and tonic clonic seizures, it also helps with bipolar disordercarbamazepinethe adverse effects of this med are CNS effects, blood dyscrasias, hypo-osmolarity (promotes secretion of ADH), and skin disorders (SJS), hepatoxicitycarbamazepinethis drug likely blocks voltage-gated sodium channels and increases GABA levelsvalproic acidthis drug is used to decrease seizure activity and prevent propagation of seizure activity, helps with all types of seizures (EVEN ABSENCE), it also helps with bipolar disorder and migraine preventionvalproic acidthe adverse effects of this med are GI effects, hepatotoxicity (anorexia, abd pain, jaundice), pancreatitis, thrombocytopenia, CNS effects (vomiting, lethargy, impaired cognitive alertness)valproic aciddon't take this drug with a carbonated beveragevalproic acidthis drug blocks transient (T-type) calcium channelsethosuximidethis drug is indicated only for absence seizuresethosuximideadverse effects of this med are nausea, vomiting, sleepiness, lightheadedness, and fatigueehtosuximidethis drug blocks voltage-gated sodium channels and increases GABAlamotriginethis drug is used for simple partial, complex partial, secondary general, tonic clonic, absence, and myoclonic seizures and also bipolar disorderlamotriginethe adverse effects of this drug are dizziness, aphasia, blurred vision, headache, N/V, depression, aseptic meningitis (headache, fever, stiff neck, N/V, sensitivity to light), skin disorders (SJS)lamotriginethis drug is a newer epileptic and inhibits presynaptic calcium channels, reducing neurotransmitter releaselevetiracetamthis drug is used for simple partial, complex partial, secondary general, tonic clonic in kids 6 and older, and myoclonic seizures,leveitracetamthe adverse effects of this drug are dizziness, weakness, agitation, anxiety, infection, nasal congestion, decreased appetitelevetiracetamthis drug is a newer antiepileptic and the action is unknown, but it affects sodium and calcium channels and also increases GABAtopiramatethe adverse effects of this drug are CNS effects, reduced sweating and increased body temp, and angle closure glaucoma, metabolic acidosis (report hyperventilation!!!)topiramatewith this drug you should monitor strenuous activity and have periodic eye examstopiramatethis drug is a newer antiepileptic and likely blocks sodium channels, and also inhibits the release of glutamateoxycarbazepinethe adverse effects of this drug are CNS effects, skin disorders (SJS), hyponatremia, multiorgan hypersensitivity reactions (fever and rash, lymphadenopathy)oxycarbazepinethis drug inhibits voltage-gated calcium channels and is a newer antiepileptic, and may increase GABA synthesisgabapentinuse this drug for nerve pain (neuropathy and herpes virus-shingles)gabapentinadverse effects of this drug are sleepiness, dizziness, ataxia, fatigue, nystagmus, and peripheral edema, but they diminish in timegabapentinthis drug is a newer antiepileptic and inhibits voltage-gated calcium channels and may change levels of neurotransmitterspregabalinthe adverse effects of this drug are nystagmus, sedation, ataxia, double vision, weight gain, peripheral edema, dry mouth, hypersensitivity reactions, fibromyalgia, peripheral edema, angioedemapregabalinwith this drug you should monitor daily weightpregabalinthese receptors go from CNS to parasympathetic ganglianicotinicthese receptors go from parasympathetic ganglia to innervated organmuscarinicnumber one cause of vasodilation isstimulation of alpha 2number one cause of vasoconstriction isstimulation of alpha 1tachycardia and increased force of contraction isstimulation of beta 1when cholinesterase is inhibited, more _________ is availabeacetylcholine