2nd class Flashcards
Zolmitriptan
A= direct selective 5-HT ID/IB receptor agonist (ser receptors) B= binds to and activates 5-HT ID/IB receptors on presynaptic trigeminal nerve endings to inhibit the release of vasodilating peptides thus preventing the stretching of stretch receptors and leading to cranial blood vessel constriction -->reducing headaches C= acute episodes of migraine
Carbamazepine
A= 1st line tricyclic antiepiletic drug B= inhibits uptake and release of NE, blocks Na+ channels which subsequently will increase the threshold for glutamate release-->decreases synaptic transmission and therefore inhibits the repetetive high frequency firing of neurons. C= generalized tonic-clonic (grand mal) seizures, partial seizures, prophylaxis of manic-depressive illness in patients unresponsive to lithium/diazepam (bipolar disorders), trigeminal neuralgia and diabetic neuropathies
Phenobarbital
A= barbiturate, sedative/hypnotic agent, antiepiletic, GABA mimetic, anxiolytic B= causes direct activation of GABAa receptors and enhances GABAa mediated current by proloning the opening of chloride ions, suppresses high-frequency firing of neurons throught the action on Na+ conductance. At high concentrations it also blocks some Ca2+ currents (L type and N type) C= insomnia, seizures (generalized tonic-clonic, partial seizures, status epilepticus)
Valproic acid (valproate)
A= GABA mimetics, 1st line broadspectrum antiepileptic, antimanic/mood stabilizer¨ B= increases GABA levels in the brain by: 1) facilitating glutamic acid decarboxylase --> enzyme responsible for GABA synthesis 2) blocks the action of GABA transaminase --> blocks degradation of GABA. Also blocks NMDA-receptor mediated excitation ---> blocks sustained high-frequency repetetive firing of neurons C= seizures, myoclonic seizures, tonic clonic seizures, bipolar disorders, migraine prophylaxis
Gabapentin
A= antiepileptic, GABA derivative
B=An increase in brain GABA concentration is observed in patients receiving gabapentin. Gabapentin is transported into the brain by the L-amino acid transporter. Gabapentin (and pregabalin) bind avidly to the α2δ subunit of voltage-gated Ca2+ channels. This appears to underlie the main mechanism of action, which is decreasing Ca2+ entry, with a predominant effect on presynaptic N-type channels. A decrease in the synaptic release of glutamate provides the antiepileptic effect.
C= partial seizures and generalized tonic-clonic seizures, neuropathic pain, focal seizures, postherpetic neuralgia, generalized anxiety disorder
Pregabalin
A= antiepileptic, GABA derivative B= transported into the brain by the L-amino acid transporter. Gabapentin and pregabalin bind avidly to the α2δ subunit of voltage-gated Ca2+ channels. This appears to underlie the main mechanism of action, which is decreasing Ca2+ entry, with a predominant effect on presynaptic N-type channels. A decrease in the synaptic release of glutamate provides the antiepileptic effect. C= partial seizures and generalized tonic-clonic seizures, neuropathic pain, focal seizures, postherpetic neuralgia, generalized anxiety disorder
Lamotrigine
A= 1st line antiepileptic, antidepressant B= prolongs the inactivation of VG Na+ channels + acts on the presynaptic Ca2+ channels-->decreasing glutamate release C= generalized tonic-clonic seizures, myoclonic seizures, partial seizures, absence seizures (petit mal seizures), lennox-gastaut syndrome, depressive stage of bipolar disorders
Ethosuximide
A= antiepileptic, cyclic ureide B= reduces the low-threshold (T-type) Ca2+current --->decreases the generation of rhytmic cortical discharge of an absence attack C= absence seizures (petit mal)
Trihexyphenidyl
A= cholinonegative drug (centrally and peripherally acting) selective m1 receptor antagonist B= blocks cholinergic activity in CNS and increases availability of dopamin---> smoother control of voluntary muscle movement + corrects the relative cholinergic excess C= reduces sialorrhoea, tremor and ridgidity --->parkinsons disease treatment
Selegilin
A= monoamine oxidase irriversible inhibitor; MAOB selective B= inhibits MAOB enzymes --> retards the breakdown of dopamine; enhances and prolongs the antiparkinsonistic effect of dopamine C= parkinsons disease
Pramiracetam
A= antidepressant, nootropic/memory enhancer, GABA mimetics
B=influences neuronal and vascular functions and influences cognitive function without acting as a sedative or stimulanT. Also acts as an allosteric modulator of the AMPA receptor. It is hypothesized to act on ion channels or ion carriers; thus leading to increased neuron excitability. Improves the function of the neurotransmitter acetylcholine via muscarinic cholinergic (ACh) receptors, which are implicated in memory processes. May have an effect on NMDA glutamate receptors, which are involved with learning and memory processes
C= cognitive impairement, e.g. after strokes, dementia, cirulation disorders, Alzheimers
Piracetam
A= nootropic/memory enhancer, GABA mimetics
B=influences neuronal and vascular functions and influences cognitive function without acting as a sedative or stimulanT. Also acts as an allosteric modulator of the AMPA receptor. It is hypothesized to act on ion channels or ion carriers; thus leading to increased neuron excitability. Improves the function of the neurotransmitter acetylcholine via muscarinic cholinergic (ACh) receptors, which are implicated in memory processes. May have an effect on NMDA glutamate receptors, which are involved with learning and memory processes
C= cognitive impairement, e.g. after strokes, dementia, cirulation disorders, Alzheimers
Phenibutum
A= nootropic agent, psychotropic, GABA mimetics
B=Phenibut exerts its effects by being an agonist at the metabotropic GABAB receptor, and at higher doses also at the ionotropic GABAA receptor.
C= cognitive impairment, posttraumatic stress disorders, anixety
Levodopa+Benserazide
A= dopamine precursor+ peripheral DOPA decarboxylase inhibitor B= allows levodopa to cross the blood brain barrier (as dopamine does not) and benserazide inhibits the metabolism of levodopa to dopamine peripherally (not centrally where Levodopa is then metabolized to dopamine) C= parkinsons disease
Memantine
A= neuroprotector (?) B= blocks NMDA receptors and thus inhibits glutamate release which is toxic in large amounts C= dementia, vascular dementia, alzheimers
