1st Class Flashcards
Nitrazepam
A= benzodiazepines
B= binds to specific GABAa recepors (btw the alpha1 and gamma2 subunits in the pentameric receptor) in CNS neuronal synapses that facilitates the frequency of GABA-mediated opening of chloride ion channel opening –> enhancing membrane hyperpolarization –> sedation and relief of anxiety, amnesia, hypnosis, anaesthesia, coma and resp depression (dose dependent depressant of CNS)
C=used for insomnia, seizures&epilepsy, relief of anxiety, for sedation and amnesia before and during surgery, as a component of combined anesthesia, for muscle relaxation in neuromuscular disorders
Triaozolam
A= benzodiazepines, short acting, Sedative – hypnotic agent
B= binds to specific GABAa recepors (btw the alpha1 and gamma2 subunits in the pentameric receptor) in CNS neuronal synapses that facilitates the frequency of GABA-mediated opening of chloride ion channel opening –> enhancing membrane hyperpolarization –> sedation and relief of anxiety, amnesia, hypnosis, anaesthesia, coma and resp depression (dose dependent depressant of CNS)
C=used for insomnia, seizures&epilepsy, relief of anxiety, for sedation and amnesia before and during surgery, as a component of combined anesthesia, for muscle, premedication(!)
Midazolam
A= benzodiazepines, short acting, Sedative – hypnotic agent
B= binds to specific GABAa recepors (btw the alpha1 and gamma2 subunits in the pentameric receptor) in CNS neuronal synapses that facilitates the frequency of GABA-mediated opening of chloride ion channel opening –> enhancing membrane hyperpolarization –> sedation and relief of anxiety, amnesia, hypnosis, anaesthesia, coma and resp depression (dose dependent depressant of CNS)
C=used for insomnia, seizures&epilepsy, relief of anxiety, for sedation and amnesia before and during surgery, as a component of combined anesthesia, for muscle, premedication(!)
Zolepidem
A= newer hypnotic drug, imidazopyridine derivative, BZ analog B= binds to specific GABAa ω2 receptors (btw the alpha1 and gamma2 subunits in the pentameric receptor) in CNS neuronal synapses that facilitates the frequency of GABA-mediated opening of chloride ion channel opening --> enhancing membrane hyperpolarization --> sedation and relief of anxiety, amnesia, hypnosis, anaesthesia, coma and resp depression (dose dependent depressant of CNS) C= sleeping disorders!
Propofol
A= hypnotic/amnesic non-barbiturate agent B= binds to specific GABAa recepors (btw the alpha1 and gamma2 subunits in the pentameric receptor) in CNS neuronal synapses that facilitates the frequency of GABA-mediated opening of chloride ion channel opening --> enhancing membrane hyperpolarization --> sedation and relief of anxiety, amnesia, hypnosis, anaesthesi C= induction anesthesia, maintenance of general anesthesia, sedation. In subanesthetic doses to treat postop nausea and vomiting
Rocuronium
A= neuromuscular blocking drug, nondepolrz muscle relaxant, steroid derivative nicotinic cholinoreceptor blocker B= acts predominantly on nicotinic receptors by competing with acetylcholine. In larger dose can also enter the pore of the ion channel to produce a more intense motor blockade. Can also block prejunctional sodium channels --> interferes with the release of acetylcholine at nerve endings C= surgical relaxation, endotracheal intubation, control of ventilation, treatment of convulsions
Sugammadex
A=Selective Relaxant Binding Agent, rocuronium antidote
B= Extensions pf the sug molecule extend the cavity size allowing greater encapsulation of the rocuronium molecule. The rocuronium molecule bound within sugammadex’s lipophilic core, is rendered unavailable to bind to the acetylcholine receptor at the neuromuscular junction.
C= agent for reversal of neuromuscular blockade by the agent rocuronium in general anaesthesia.
Neostigmine
A= cholinopositive drug, indirect acting parasympathomimetics, reversible anticholinesterase (carbamate + modest direct acting property; activates nicotinic receptors too) B= blocks enzymes cholinersterases (ACHE and butyrylcholinesterase) by forming covalent bonds with them --> evokes prolonged effects of acetylcholine in the synaptic cleft--> stimulates N and M receptors through the activity of ACE C= glaucoma(physostigmine), myasthenia gravis(improves muscle tone), decurarization (reversal of anticholinergic effects), muscle paralysis, atony of guts and bladder, central paralysis
Morphini hydrochloridum
Morphini sulfas
A= phenanthrene opioid agonist, analgesic, sedative agent
B= binding to and activating the μ-opioid receptors in the
central nervous system. Activation of the μ-opioid receptors is associated with analgesia,
sedation, euphoria, physical dependence and respiratory depression. (by agonizing the receptor the opioid close voltage gated ca2+ channels on presynaptic neurons–> reduce transmitter release as well as hyperpolarize and thus inhibit postsynaptic neurons by opening K+ channels)
C= cough in terminal disease, acute pain, severe pain premedication, postoperative pain, myocardial infarction, acute pulmonary oedema, chronic severe pain in palliative care, adjunct to rehydratation in acute diarrhoea.
Fentanyl
A= Synthetic narcotic analgesics, opioid agonist, phenylpiperidines
B= binding to and activating the μ-opioid receptors in the
central nervous system. Activation of the μ-opioid receptors is associated with analgesia,
sedation, euphoria, physical dependence and respiratory depression. (by agonizing the receptor the opioid close voltage gated ca2+ channels on presynaptic neurons–> reduce transmitter release as well as hyperpolarize and thus inhibit postsynaptic neurons by opening K+ channels)
C= cough in terminal disease, acute pain, severe pain premedication, postoperative pain, myocardial infarction, acute pulmonary oedema, chronic severe pain in palliative care, adjunct to rehydratation in acute diarrhoea. neiroleptanalgesia
Tramadol
A= centrally acting analgesic, opioid agonist, antidepressant B= weak u-opioid agonist, moderate SERT inhibitor and ser releasing agent, weak NET inhibitor, NMDA receptor antagonist, 5HT2c antagonist --> depresses cns and promotes anti depressive effect C= moderate to severe pain, chronic pain syndromes, depression and OCD
Buprenorphine
A= partial opioid receptor agonist, kappa receptor antagonist, phenanthrene derivative, analgesic agent
B= partial agonist at opioid receptor and antagonizes kappa receptors. Also binds ORL1 receptors (orphanin receptor)
C=detoxification and maintenance of heroin abuse, management of opioid dependence, chronic pain
Methadone hydrochloride
A= analgesics, opioid receptor agonist
B= slow-acting agonist of u opioid receptor—> Activation of the μ-opioid receptors is associated with analgesia,
sedation, euphoria, physical dependence and respiratory depression. (by agonizing the receptor the opioid close voltage gated ca2+ channels on presynaptic neurons–> reduce transmitter release as well as hyperpolarize and thus inhibit postsynaptic neurons by opening K+ channels)
C= substitution therapy for opioid addicts, prevents withdrawal symptoms, chronic severe pain
Naloxone hydrochloride
A= competetive opioid receptor antagonist B= nonselectively antagonizes opioid receptors --> reverses the acute effects of opioids--> can precipitate severe abstinence syndrome C= opioid overdose, alcohol and opioid addiction
Naltrexone hydrochloride
A= opioid receptor antagonist B= antagonizes opioid receptors --> blocks the effects of opioids. It displaces the morphine, heroin and other opiates from gamma receptors and bounds them closely than agonist do. C= treatment of alcoholism, opioid overdose (antidote)
Paracetamol (US: acetaminophen. antidote in case of poisoning; acetylcysteine)
A= non-opioid analgesic, antipyretic B= inhibits COX-1 and COX-2 enzymes in peripheral tissues (without anti-inflammatory properties). COX normally converts the fatty acid arachidonic acid into endoperoxidase, prostaglandins and thromboxanes. C= treatment of mild to moderate pain: headaches, myalgias, postpartum pain
Metamizole (US: dipyrone)
A= pyrazolone derivative, non-opiod analgesic, antispasmodic, antipyretic, (short term painkiller)
B= blocks COX-1 and COX-2 enzymes–>inhibits production of prostaglandins and other inflammatory mediators
C=perioperative pain, acute injury, cancer induced pain, other acute/chronic forms of pain and high fever unresponsive to other agents.
Acamprosate
A= NMDA (NmethylDaspartat4e) glutamate receptor antagonist B= blocks NMDA receptors-->preventing the excitatory transmittor glutamate from binding to them and activates GABAa receptors---> reduces the desire of alcohol intake C= treatment of chronic alcoholism (reduces risk of relapse)
Disulfiram
A=acetaldehyde dehydrogenase inhibitor
B= causes extreme discomfort in people who drink alcoholic beverages (when taken with alcohol!) by inhibiting aldehyde dehydrogenase –>alcohol is metabolized as usual but acetaldehyde is accumulating and producing the discomfort effects
C= alcohol dependence treatment
Clonidine
A= adrenopositive drug, selective alpha2 presynaptic receptor agonist B= binds to and activates presynaptic alpha2 receptors --> located on cardiovascular control centers--> decreasing impulsation among sympathetic nerves from CNS--> decreasing of bp. Blood vessels--> decreased release of NE and decreasing of bp C= hypertension, hypertensive crisis when immideate effects are not necessary. Differential diagnosis of pheochromocytoma in hypertensive patients, prophylaxis of vascular migraine headaches, ADHD. Painkiller properties, reliefs withdrawal symptoms of opioids or alcohol abuse
