Pharmacology Flashcards
Agonists
Drugs that mimics a naturally occurring substance to stimulate a specific receptor
Antagonist
Drug binds to a receptor without activating it in order to block other potential substances from activating the receptor
Therapeutic Index
TD/ED (toxic dose in 50% of subjects / effective dose in 50% of subjects)
Pharmokinetics
The process by which a drug is absorbed, distributed, metabolized, and eliminated by the body
Metabolism
Deactivation by the liver with GI tract and other organs breaking the drug down to a less extent
Elimination/excretion
Primarily by the kidneys
Clearance
Volume of plasma from which a drug is eliminated per unit time
Half-life
Time required to reduce the plasma drug concentration by 50%
Decreased metabolism
- Decreased clearance
- Increased half life
- Increased plasma
Increased metabolism
- Increased clearance
- Decreased half life
- Decreased plasma
Mechanisms of anti-psychotics towards managing agitation
Inhibiting dopamine transmission
Typical anti-psychotics
- Cholorpromazine
- Haloperidol
- Perphenazine
- Fluphenazine
Second generation medications (“atypical”) treat…
- Depressive states
Adverse effects of psychotics
- Rigidity, tremors
- TD
- OH
- Change in weight, glucose/lipid levels
- Dizziness
Benzodiazepines (treat + mechanism)
- Treat anxiety, seizures, spasticity, anesthesia, sedative
- Binds to GABA receptors to cause hyper-polarization and inhibit neuronal firing
- *Can lead to physical dependence, withdrawal symptoms
Benzodiazepines ending
“-AM”
- Estazolam
- Flurazepam
- Queazepma
- Clonazepam
Non-benzo meds = Barbituates (treat + mechanism)
- Use to promote sleep, also a good anesthetic
- Binds to GABA receptors = cause decreased arousal and increased sleepiness
- *HIGHLY ADDICTIVE with small therapeutic index
Barbituates ending
“-AL”
- Amobarbital
- Phenobarbital
- Pentobarbital
Most commonly prescribed non-benzos
- Zaleplon (Sonata)
- Zolpidem (Ambien)
- Eszopiclone (Lunesta)
Precedes (treat + mechanism)
- Used as a sedative in ICUs to control agitation
- Binds to alpha-2 receptor to decreased sympathetic response
- *May cause bradycardia or hypotension
Partial seizure
Simple - may cause motor, sensory, autonomic,or psychological symptoms without obvious change in consciousness
- Complex - focal seizure activity with impaired consciousness
- *May spread across hemispheres and become generalized
Generalized seizure
- Simple - brief loss of consciousness without any detectable signs
- Complex - loss of consciousness with notable clinical signs present
- Absence (petit mal) - brief lapses without loss of postural control
- Tonic-clinic - loss of consciousness with violent muscle contractions
First-line medications of partial seizures
- Carbamzepine (Tegretol)
- Phenytoin (Dilantin)
- Oxcarbazepine (Trileptal)
- Valproic acid (Valproate)
FIrst-line medications for generalized tonic-clinic seizures
- Valproic acid (Valproate)
- Lamotrigine (Lamictal)
- Topiramate (Topamax)
Anti-seizure mechanism of action and side effects
Mechanism - blockaded of voltage gated sodium channels Common side effects - Nausea - Dizziness - Poor coordination - Drowsiness/sleepiness - Diplopia
Neurostimulants mechanism
- Increases synaptic concentration of dopamine, serotonin, and non-adrenaline
- Increases neuronal sprouting and synaptogensis
- Increases synaptic efficiency by facilitating long-term potentiation
Neurostimulant types
- Ritaline
- Amphetamine
- DA agonists
Tizanidine (mechanism + treat)
- Centrally acting alpha-2 adrenergic agonists which decreases polysnynaptic reflex activity
- Used in conditions of marked muscle weakness
Tizanidine side effects
- Hypotension
- Elevated liver enzymes
- Sedation
- Hallucinations
Baclofen (mechanism + treat)
- Acts centrally by binding to GABA receptors and inhibits spinal reflexes
- Used when muscle weakness is not severe
Baclofen side effects
- Sedation
- Muscle weakness
- Confusion
- Dyskinesia
- Hallucinations
Diazepam (Benzo) (mechanism + treat)
- Centrally acting by inhibiting GABA receptors and pre-synaptic/postsynaptic reflexes
- Used with painful spams especially at night
Diazepam side effects
- Sedation
- Habituation
Dantrolene sodium (mechanism + treat)
- Acts directly on skeletal muscle by prevention release of calcium from SR
- Used with severe spasms and spinal cord lesions
Dantrolene sodium side effects
- Weakness
- Diarrhea
- Hepatotoxicity
Clonodine (mechanism, treat, + side effects)
- Decreases polysynaptic reflex activity
- Used with spasticity associated with uncontrolled HTN
- Side effects: OH
Gabapentin (mechanism, treat, + side effects)
- Similar structure to GABA, mechanism unknown
- Used with MS and SCI
- Side effects: sedation, confusion, fatigue, weight gain
Botox (mechanism + lasting effects)
- Acts on NMJ by inhibiting release of ACH at pre-synaptic terminal
- Effects last for 2-6 months
