Trans 047 Pharma Doc Torres Flashcards
• Old sedatives • Category D drugs in pregnancy
barbiturates
contraindications to barbiturates?
Contraindications: Porphyria
most common AE of barbiturates is
porphyria
an attack of porphyria may manifest as?
an attack, manifested by severe abdominal pain, nausea, vomiting, psychiatric disorders, and neurologic abnormalities.
DOC for Febrile Epilepsy?
barbiturates
only barbiturates available in the PH. long acting?
PHENOBARBITAL
short acting barbiturates?
pentobarbital
intermediate acting barbiturate?
secobarbital
Evidence of human fetal risk has been documented, but the benefits to the mother may be acceptable despite the risk to the fetus. Drugs in this class may be used in pregnancy if the benefits to the mother outweigh the risk to the fetus (i.e. a life threatening situation or a serious disease for which safer medication cannot be used or are not efficacious). Examples of medications in this class are phenytoin, valproic acid and phenobarbital.
what category of drug?
Category D
Studies in animals have revealed adverse effects on the fetus and there are no controlled studies in women, or studies in women and animals are not available. Drugs from this class can be given to pregnant women if the benefit to the mother outweighs the risk to the fetus. Examples of medications in this class are diltiazem and spironolactone.
what category
category C
Bind selectively to a subgroup of GABA-A receptors, acting like benzodiazepines to enhance membrane hyperpolarization
what drug?
benzodiazepine GABA A
which benzodiazepine GABA A:
• No active metabolites • Available in 5-10 mg per ta
Zolpidem
which benzodiazepine GABA A:
• Inhibit aldehyde dehydrogenase • 5-20 mg per capsule
Zaleplon
which benzodiazepine GABA A:
• Minor active metabolite
• Available in 1-3 mg per tablet
Most potent
Eszopiclone
- Anxiolytics – treatment for anxiety
* Category B drugs in pregnancy
5-HT-1A AGONISTS
a serotonin receptor subtype located in presynaptic and postsynaptic membranes.
5-HT-1A
Either animal‐reproduction studies have not demonstrated a fetal risk but there are no controlled studies in pregnant women, or animal studies have demonstrated risk to the fetus that was not confirmed in controlled studies in pregnant women in the first trimester and there is no evidence of a risk in later trimesters. Medications in this class are generally considered safe. Examples of medications in this class are acetaminophen and amoxicillin
what category?
Category B
which 5HT1A?
Most commonly used and the only one available in the Ph
• 5-10 mg per tablet BID/TID
relieves anxiety without causing marked sedative, hypnotic, or euphoric effects.
Buspirone
Before, it was an herbal plant, now it is approved as a hypnotic Activates MT1 and MT2 receptors in suprachiasmatic nuclei in the CN. Promotes rapid onset of sleep with minimal rebound insomnia or withdrawal symptoms
M1-M2 Agonist (melatonin)
• DOC for Insomnia and Jetlag • 8 mg per tablet • Category C drugs in pregnancy
Ramelteon (M1-M2 Agonist)
Most commonly used sedative
Most potent but non-addicting • Toxic dose – 100 mg
BENZODIAZEPINE GABA-Cl (Chloride)
MOA benzodiazepine GABA cl
MOA: Bind to specific GABA-A receptor subunits at central nervous system (CNS) neuronal synapses facilitating GABA-mediated chloride ion channel opening frequency. Also enhance membrane hyperpolarization
antidote for BENZODIAZEPINE GABA-Cl (Chloride)
FLUMAZENIL (BDZ-Antagonist)
approved for use in reversing the CNS depressant effects of benzodiazepine overdose and to hasten recovery following use of these drugs in anesthetic and diagnostic procedures. MOA: Antagonist at benzodiazepine binding sites on the GABA-A receptor
FLUMAZENIL (BDZ-Antagonist)
BENZODIAZEPINE GABA-Cl (Chloride) has Additive depressant effects with:
Additive depressant effects with: Alcohol, Anti-H1 (anti-histamine), Anti-HPN When added to alcohol, it causes more depression that’s why additive effect
BENZODIAZEPINE GABA-Cl (Chloride) that is
active?;
very active?
CHLORDIAZEPOXIDE
DIAZEPAM
BENZODIAZEPINE GABA-Cl (Chloride) that is
• Long half-life
FLURAZEPAM
BENZODIAZEPINE GABA-Cl (Chloride) that is
Rapid-acting; most rapid ?;
slow acting? ;
Short-acting; shortest
Commonly used in the elderly
alprazolam
temazepam
Triazolam
BENZODIAZEPINE GABA-Cl (Chloride) that are pro drug?
CLORAZEPATE
OXAZEPAM
LORAZEPAM
NITRAZEPAM
peptides found in specific hypothalamic neurons that are involved in the control of wakefulness and that are silent during sleep.
increase in the day and decrease at night.
Loss of this neurons is associated with narcolepsy, a disorder characterized by daytime sleepiness and cataplexy. Animal studies show that orexin receptor antagonists have sleep-enabling effects.
OREXIN A and B
Blocks binding of orexins, neuropeptides that promote wakefulness, thus, promoting sleep onset and duration.
Newer hypnotic drugs
• AE: Somnolence
Orexin Antagonist
Example of Orexin Antagonist
SUVOREXANT / Almorexant
Old drug but still used today • Cyclic ureides • Blocks Na, K, and Ca channels • GABA potentiators (inhibitory) • AE (oral): gingival hyperplasia
PHENYTOIN ORAL / FOSPHENYTOIN IV
a sodium channel-blocking antiseizure drug that acts in a similar fashion to carbamazepine and other agents in the class.
is effective in preventing focal onset seizures and also tonic-clonic seizures, whether they are focal-to-bilateral tonic-clonic (secondarily generalized) or occurring in the setting of an idiopathic generalized epilepsy syndrome.
PHENYTOIN ORAL / FOSPHENYTOIN IV