First Aid Pharm - Neuro

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NEUROLOGY PHARMACOLOGY

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What is the underlying cause of Parkinson's?

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loss of dopaminergic neurons and excess cholinergic activity

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Mneumonic for Parkinson's Disease drugs?

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BALSA: Bromocriptine, Amantiadine, Levodopa (+carbidopa), Selegiline (+COMT inhibitors), Antimuscarinics

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MOA of Bromocriptine?

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agonize dopamine receptors (ergot alkaloid and partial dopamine agonist)

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Agents that increase dopamine?

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Amantadine (increase dopamine release), L-dopa/carbidopa(converted to dopamine in CNS)

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MOA of Selegiline and entacapone/tolcapone?

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Prevent dopamine breakdown (Selegiline=selective MAO type B inhibitor)and (entacapone/tolcapone=COMT inhibitors)

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MOA of Benztropine?

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Curbs excess cholinergic activity (antimuscarinic)

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Antimuscarinic that improves tremor and rigidity but has little effect on bradykinesia?

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Benztropine

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Clinical use of L-dopa/carbidopa?

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Parkinsonism

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MOA of L-dopa/carbidopa?

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Increase dopamine levels in brain. Cross BBB and converted by dopa decarboxylase in CNS to dopamine.

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Toxicity of L-dopa?

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Arrhythmias from peripheral conversion to dopamine; dyskinesia after doses and akinesia between doses.

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How can you avoid L-dopa induced arrhythmias?

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Give with carbidopa = a peripheral decarboxylase inhibitor

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Selegiline MOA?

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Inhibits MAO-B; increase dopamine availability

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Selegiline toxicity?

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enhance adverse effects of L-dopa

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Sumatriptin MOA?

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5-HT1D agonist. Causes vasoconstriction.

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Clinical use of Sumatriptin?

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acute migraine, cluster headaches

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Sumatriptin toxicity and contraindications?

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coronary vasospasm; contraindicated in pts with CAD or angina

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Clinical use of phenytoin?

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1st line for generalized tonic-clonic seizures and status epilepticus prophylaxis. Also a class IB antiarrhythmic.

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MOA of phenytoin?

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increase Na+ channel inactivation. Inhibits glutamate (excitatory) release.

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Clinical use of Carbamazepine?

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1st line for generalized tonic-clonic seizures and trigeminal neuralgia. Also for simple and complex partial seizures.

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MOA of Carbamazepine?

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increase Na+ channel inactivation

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Toxicity of Carbamazepine?

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diplopia, atazia, agranulocytosis, aplastic anemia, liver toxicity, teratogenesis, induces cyto P-450

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Toxicity of phenytoin?

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nystagmus, diplopia, ataxia, sedation, gingival hyperplasia, hirsutism, megaloblastic anemia, teratogenesis, malignant hyperthermia, SLE-like syndrome, induces cyto P-450

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Lamotrigine MOA?

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blocks voltage-gaated Na+ channels

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Clinical use Gabapentin?

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simple and complex partial seizures; generalized tonic-clonic. Also peripheral neuropathy.

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MOA of Gabapentin?

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increase GABA release

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Topiramate MOA?

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blocks Na+ channels, increase GABA action

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Gabapentin toxicity?

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sedation, ataxia

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Lamotrigine toxicity?

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Stevens-Johnson syndrome.

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Topiramete toxicity?

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sedation, mental dulling, kidney stones, weight loss

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Phenobarbital clinical use?

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1st line in preggers and kids. Generalized tonic-clonic and simple and complex partial seizures.

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Barbituate toxicity?

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sedation, tolerance, dependence, cyto P-450 induction, resp/CV depression, additive with alcohol

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Barbituate MOA?

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increases GABA-A action by increase DURATION of Cl- channel opening, which decreases neuron firing. [barbiDURATe=increased DURATion]

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Valproic acid clinical use?

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1st line for generalized tonic-clonic seizures. Also for myoclonic and absence seizures.

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Valproic acid MOA?

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increase Na+ channel inactivation. Increase GABA concentration.

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Valproic acid toxicity?

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GI distress, fatal hepatotoxicity, neural tube defects, tremor, weight gain

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Ethosuximide clinical use?

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1st line for absence seizures.

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MOA ethosuximide?

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blocks thalamice T-type Calcium channels

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Ethosuximide toxicity?

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GI distress, lethargy, headache, urticaria, Stevens-Johnson syndrome

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Benzodiazepine clinical uses?

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1st line for acute status epilepticus; also for seizures of eclampsia

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Name 4 barbituates.

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Phenobarbital, pentobarbital, thiopental, secobarbital

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Barbituate contraindication?

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porphyria

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Name some Benzodiazepines. (8)

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diazepam, lorazepam, triaxolam, temazepam, oxazepam, midazolam, chlordiazepoxide, alpraxolam

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MOA of Benzos?

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Facilitate GABA-A action by increse FREQUENCY of Cl- channel opening

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What drug class do you use for alcohol withdrawal-DTs?

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Benzos

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What are the 3 short-acting Benzos?

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TOM thumb= Triazolam, Oxazepam, Midazolam

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Do benzos or barbituates have a higher risk of resp depression and coma?

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Barbituates

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How do you treat a Benxo overdose?

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Flumazenil (competitive antagonist at GABA receptor)

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Name 6 inhaled anesthetics

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halothane, enflurane, isoflurane, sevoflurane, methoxyflurane, nitrous oxide

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Effects of inhaled anesthetics?

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myocardial and resp depression, nausea/emesis, increase cerebral blood flow

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Toxicity of halothane, methoxyflurane, and enflurane?

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hepatotoxicity (halothane), nephrotoxicity (methoxyflurane), proconvulsant (enflurane)

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Drug classes used as IV anesthetics? (5)

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Barbiturates, Benzos, Ketamine, Opiates, Propofol

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Name the local anesthetics that are esters

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procaine, cocaine, tetracaine, amides

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Name the local anesthetics that are amides

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lidocaine, mepivacaine, bupivacaine

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barbiturate used as IV anesthetic?

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thiopental - used for short surgical procedures and induction of anesthesia

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drug used for endoscopy?

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midazolam

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Arrylcyclohexamine (ketamine) effects?

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CV stimulant, disorientation, hallucination, bad dreams, increase cerebral blood flow

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Opeates used during general anesthesia?

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morphine, fentanyl

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MOA of local anesthetics?

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block Na+ channels. Tertiary amines penetrate membrane in uncharged form, then bind to ion channels as charged form.

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Order of nerve block?

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small diameter>large diameter. Myelinated>unmyelinated. Size predominates over myelination.

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order of loss during nerve block?

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pain(1st)>temp>touch>pressure

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how do you enhance local action?

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give with vasoconstrictors (EPI)

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What happens to local anesthetics in infected tissues?

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tissue is acidic; anesthetics are charged and can't penetrate membrane. More anesthetic is needed.

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What receptor do neuromuscular blocking drugs target and what are they used for clinically?

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motor (vs. autonomic) nicotinic receptor. Used for muscle paralysis in surgery or mechanical ventilation.

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Depolarizing neuromuscular blocking drug?

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succinylcholine

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nondepolarizing neuromuscular blocking drugs?

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tubocurarine, atracurium, mivacurium, pancuronium, vecuronium, rapacuronium

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What is dantrolene used for?

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treatment of malignant hyperthermia and neuroleptic malignant syndrome

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MOA of dantrolene?

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prevents release of calcium from the SR of skeletal muscle

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How do you reverse blockade of nondepolarizing neuromuscular blocking drugs?

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neostigmine, edrophonium, and other cholinesterase inhibitors