Pharmacology V Flashcards
Antianxiety Medications are also known by what 2 other names?
Sedative hyponotics
Minor tranquilizers
What class of drugs, among the most widely used in medicine, is diazepam (Valium) a part of?
Benzodoazepines
Valium
diazepam
T/F
All benzodiazepines have the same basic structure of 2 nitrogens (diazo) and a benzene ring that binds GABA receptors
True
Name 4 Benzodiazepines used in Dentistry for pre-op anxiety:
diazepam (Valium)
lorazepam (Ativan)
alprazolam (Xanax)
midazolam (Versed)
Benzodiazepines are Schedule _____ opiates in the US, are highly addictive and also exhibit _______.
IV/V
Tolerance
Name 3 distinct effects of Benzodiazepines:
Effects on behavior
Anticonvulsant effects
Muscle relaxation
Benzodiazepines have ________ effects at low doses and ________ at high doses.
Anxiety reduction
Drowsiness/depression
Anesthetic-induced seizures in dentistry can be prevented by and arrested by what 2 Anticonvulsants?
diazepam (Valium)
midazolam (Versed)
What are the 2 most potent Benzodiazepines?
diazepam (Valium)
chlordiazepoxide (Librium)
Aside from depressing motor nerve and muscle function in healthy pts and ones with skeletal muscle disorders, Benzodiazepines are predatory drugs that cause _______.
Anterograde Amnesia
Describe the mechanism of the Benzodiazepines.
3 things
Enhances inhibitory effect of GABA on neuronal excitability
Causes hyperpolarization (less excitable state)
Neuronal stabilization
What does GABA do to the brain?
Inhibitory
Decreases Excitation
At the level of the synapse, the GABA receptor binds both ______ and ______.
GABA
Benzodiazepines
What can enhance the binding effect of Benzodiazepines at the synapse?
Presence of GABA
*binding is rapid, reversible, stereospecific, and saturable
Most Benzodiazepines have very long _______ and are metabolized in the ______ compounds
half lives
active
Due to the fact the drug is metabolized rapidly to inactive compounds, what Benzodiazepine is a very good choice for Dentistry?
lorazepam (Ativan)
*No significant accumulation of drug do to rapid metabolization
What Benzodiazepine has the shortest half life of the Oral meds and has increased psychomotor impairment and risk of oversedation in the elderly?
triazolam (Halcion)
Name 5 uses of Benzodiazepines in Medicine:
Anxiety relief
Muscle relaxant
Insomnia
Alcohol withdrawal
Pre-op med
What are 3 used of Benzodiazepines in Dentistry:
Pre-op med (for anxiety)
IV sedation (and amnesia)
Emergency intervention for seizures
Name 4 adverse side affects of Benzodiazepines:
CNS depression
Xerostomia
Abuse/addiction
Additive with other CNS depressants (alcohol)
T/F
Parenteral administration of Benzodiazepines causes acute hypotension, muscle weakness, apnea, and can cause cardiac arrest
True
When using Benzodiazepines in conjunction with Opiates, how much should the normal dose of the Opiate be reduced?
1/3
What DDI is most dangerous with Benzodiazepines, resulting in significant Respiratory Depression?
Alcohol
*must be avoided
Why must alcohol be avoided for days after taking a dose of Benzodiazepine?
long half lives
What is the 1/2 life of Valium?
active metabolite of desmethyldiazepam?
20-50 hrs
50-100 hrs
*why EtOH must be avoided
What is the antidote for Benzodiazepine Overdose?
*this antidote will not block CNS effects from other drugs
Flumazenil
Flumazenil (antidote for Benzodiazepine overdose) may not reverse ________.
It may cause _______ as a side effect.
Respiratory depression
seizures
Name a “miscellaneous Anti-anxiety Agent” used to manage generalized anxiety disorder (no known mechanism)
buspirone (BuSpar)
buspirone (BuSpar) causes many DDI’s in dentistry (antibiotics, antifungals) that will increase its concentration and is considered a ________ in dentistry
Red Flag Drug
Antidepressants and Anti-anxiety meds cause ________, which is particular interest in dentistry
Xerostomia
Throwback: SSRI’s cause what to the teeth?
Bruxism
Major Tranquilizers are known as ________ medications and the older term is ________ drugs.
Antipsychotic
Neuroleptic
Name 2 indications for the use of a Major Tranquilizer:
Psychotic disorders (pchizophrenia, paranoia)
Demetia
What is a side effect to Major Tranquilizers?
Severe nausea and vomiting
Major Tranquilizers act as _______ to a swath of neurotransmission
(dopaminergic, alpha 1 and 2 adrenergic, srotonergic, muscarinic, H1 histamine, sigma opioid)
Antagonists
T/F
The primary mechanistic action of Major Tranquilizers is the blockage of dopaminergic transmission
True
*one hypothesis is that Schizophrenia is caused by an overactivity of the dopaminergic system
The blockage of Dopamine by Major Tranquilizers has what 3 important effects?
Antipsychotic
Extrapyramidal side effects
Antiemetic (anti-vomit)
Antipsychotic medications reduce Dopaminergic activity by blocking _____ receptors
D2
T/F
All Major Tranquilizers are strong D2 dopamine receptor agonists with one exception - clozapine (Clozaril)
False
Antagonists
If the receptors are blocked within 2-4 hours after Major Tranquilizers are administered, what is then the problem with the Dopaminergic Hypothesis?
Aside from this, schizophrenia is also associated with alterations in neural structure in the limbic system and the ______.
Therapeutic activity takes weeks for full effect
Prefrontal cortex
The new thought is that Major Tranquilizers, instead of acting to alleviate schizophrenia by turning down dopamine, helps to recover normal cell ________.
Morphology
T/F
All Major Tranquilizers have similar pharmokinetics and Efficacy
True
1/2 life = 18-40 hrs, once daily dosing
Name 5 Extrapyramidal side effect of Antipsychotic Drugs:
Parkinsonism (akinesia - difficult initiating movement)
Akathisia (restless leg)
Dystonia (sustained muscle contraction)
Tardive Dyskinesia (abnormal face/tongue movements)
Sedation
_________ drugs can treat most Extrapyramidal side effects of Antipsychotic Drugs
Anticholinergic
The Sedation side effect of Antipsychotic Drugs manifests itself how (as a result of histamine, cholinergic, and adrenergic blockage)
Autonomic Side Effects
Antipsychotics potentiate (exacerbate) the ________ caused by opioids.
***potentiate CNS effects of all analgesics
Respiratory Depression
Name 3 Dental considerations with Antipsychotics?
Hematologic (WBC count may be low)
Heart (arrhythmias - caution with epi)
Extrapyramidal (movement)
An episode of neurologic dysfunction, often accompanied by motor activity such as convulsions, and emotional/sensory change
*may contain visual, auditory, and olfactory hallucinations
Seizure
The majority of patients suffering from seizures have _______ epilepsy.
Idiopathic
*no known cause
Drugs improve epilepsy in __-__% of cases
70-80%
What are 2 broad groups of epilepsy?
Partial
Generalized
What are the 2 subtypes of Partial Epilepsy
Briefly describe them:
Simple Partial - Single group hyperactive neurons. Few seconds, no loss of consciousness, often single limb/muscle group abnormal
Complex Partial - Hallucinations, Mental distortion, AURA (lasting 3-5 minutes). Full consciousness slow to return
In a Complex Partial Seizure, the Aura lasts for _____ minutes.
They are also known as ________ seizures
_____% of people with complex partial epilepsy experience their initial seizure prior to 20
3-5
temporal lobe
80
What are the 2 types of Generalized Epilepsies?
Tonic-clonic (grand mal)
Absence (petit mal)
In both Tonic-clonic (grand mal) and Absence (petit mal) Generalized Epilepsies, _______ is lost.
Consciousness
______ is producing/restoring normal tone of continuous tension, _______ is contraction/relaxation of muscles.
Tonic
Clonic
In a Tonic-Clonic (grand mal) seizure, Major Motor Activity is involved and during the seizure ________, and consciousness returns with exhaustion, headache, drowsiness, and _______.
Comatose
Confusion
A brief period of heightened sensory activity prior to the onset of a seizure characterized by numbness, nausea, or sensitivity to light, odor, or sound.
Aura
Absence (petit mal) seizures are usually found in what demographic?
Describe a petit mal seizure:
Childred 3-5 yrs
No aura, rapid eye blinking 3-5 seconds, quickly return to normal
What life-threatening condition is characterized by seizures that are continuous or rapidly recurrent?
If this occurs in a dental office, what should be given?
Status Epilepticus
diazepam (Valium) injection
*lorazepam (Ativan) and midazolam (Versed) also can be used
T/F
Drugs have variable efficacy in the treatment of seizures
True
Drugs for Epilepsy are generally ___________, and prevent the spread of abnormal electric discharges in the brain without causing excessive drowsiness
CNS depressants
Most anticonvulsants have a Narrow/Large therapeutic index.
They tend to stimulate ________ enzymes, thus these drugs are known as _______.
Narrow
Liver microsomal
Inducers
***the addition of an anticonvulsant will change the metabolism of all anticonvulsants
T/F
Metabolism of anticonvulsants can saturate liver microsomal enzymes
- low dose - 1st order
- saturation - zero order
- thus at saturation, even a small change in dose can leade to large increase in blood level of dose
True
Name 2 major side effects of Anticonvulsants:
Name 2 ways these side effects affect Dental Decisions:
CNS depression, GI effects
Opioids and Benzodiazepines Additive (CNS), NSAIDS may exacerbate GI irritation
What drug that blocks Sodium channels is highly effective for simple and complex partial seizures?
carbamazepine (Tegretol)
carbamazepine (Tegretol) blocks _____ channels and is highly effective for ______ and _______ seizures.
sodium
simple
complex partial
Other than treating seizures, carbamazepine (Tegretol) has what 3 clinical uses?
(One of very special interest in Dentistry)
Bipolar depression
Chronic pain
Trigeminal neuralgia (tic douloureux)
What are 4 side effect of carbamazepine (Tegretol)?
Hematologic
Liver Toxicity
Congestive heart (altered BP)
Xerostomia
carbamazepine (Tegretol) is a classic Inducer, which means…
Decreases effectiveness of a variety of drugs
warfarin, doxycycline, oral contraceptives, asthma bronchodilators
T/F
carbamazepine (Tegretol) DDI’s include macrolides, which increase the former’s blood levels and the hepatotoxicity of acetaminophen
True
What drug reduces the frequency of seizures by decreasing neuronal membrane passage of sodium ions thereby having a stabilizing effect?
phenytoin (Dilantin)
***remember, carbamazepine (Tegretol) blocks Na channels completely
What are 3 anticonvulsant applications of phenytoin (Dilantin)?
***What is 1 Dental Application?
Partial seizures
Tonic-Clonic seizures
Status Epilepticus
***Trigeminal neuralgia
Other than Gingival Hyperplasia, what are 2 dental side effects of phenytoin (Dilantin)?
(1 has to do with Vitamin D/folate deficiencies, which leads to osteoporosis)
Loss of taste
oral mucosal ulceration or glossitis from Folate deficiency
What % of pts taking phenytoin (Dilantin) experience Gingival Overgrowth?
What reduces the severity?
50-60%
Good Oral Hygiene
phenytoin (Dilantin) is Teratogenic category D, and causes what?
How does this manifest?
Fetal Syndrome
cleft lip, palate, congenital heart disease
phenytoin (Dilantin) has many DDI’s, ______ the metabolism of many drugs, and is a ________ of cytochrome P450
Increases
Inducer
What type of agents Inhibit the release of Acetylcholine from the presynaptic neuron?
What do they release?
GABAmimetic Agents
GABA from presynaptic interneurons
How do GABAmimetic agents prevent seizures?
Prevent acetylcholine release
*many seizures caused by tremendous release of acetylcholine
GABA is Inhibitory/Excitatory?
Inhibitory
Anticonvulsant that reduces the Na and K transport along axonal membranes and Potentiates the Inhibitory effects of GABA-mediated neurons?
phenobarbital (Luminal)
What is the most common barbiturate used as an anticonvulsant?
phenobarbital (Luminal sodium)
What types of seizures dos phenobarbital (Luminal sodium) prevent?
Tonic-clonic
Partial seizures