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Pharmacology
Chapter 11
Question | Answer |
---|---|
When should the dental health care provider asses the pt.'s anxiety? | On both first and subsequent visits. |
Why will the health care provider use orally administered drugs to provide relaxation for an anxious pt. and not use (IV) administration? | Most states require separate certificates for (IV) or conscious sedation. |
In the largest dose given of Sedative-Hypnotic Agents, what is produced? | General anesthesia and death. |
What level of the Sedative-Hypnotic Agents, produce the anxiolytic effect? | Small dose |
What agents can produce varying degree of the CNS depression, depending on the dose administered? | Sedative-Hypnotic Agents |
What do small doses of Sedative-Hypnotic Agents produce? | CNS depression (sedation), reduction of activity, and simple anxiety. |
What do the large doses of Sedative-Hypnotic Agents do? | Produce CNS depression in greater amounts. |
T/F Benzodizapines are named according to their reactions. | False-the structures are what combines them together in a group. |
What two Benzodiapines were named in Dr. Dawson's lecture? | Chlordiazepoxide (Librium) and Diazepam (Valium) |
In what forms are Benzodizapines available? | Tablets, capsules, oral solutions, rectal gel, and injectable form. |
When Benzodizapines are administered by the oral route they are well absorbed and the onset of action is related to their lipid solubility. First is true, second is false; both are true; both are false; first is false, second is true | Both are true |
What route of Benzodizapines are administered that produce a rapid and predictable response that is ideal for conscious sedation? | IV administration |
What does the Benzodizapines cross to produce an effect on the CNS and the fetus? | Blood-brain barrier and placental barriers |
Benzodizapines enhance or facilitate the action of what neurotransmitter, that is a major inhibitory transmitter in the CNS? | GABA y-aminobutyric acid, the inhibitor is enhanced |
T/F The clinical effects in humans are anxiety and panic reduction at low doses and drowsiness and even sleep at higher doses belong to the Antiseizure Effects section. | F- Behavioral effects; Antiseizure effects increase the seizure threshold. |
Muscle Relaxation can produce relaxation of what? | Skeletal Muscle |
In general Benzodizapines are what? | Used alone, have a wide margin of safety, similar adverse effects, but differ in their frequency. |
What are the most common side effects of Benzodizapines? A. CNS depression B. Fatigue C. Drowsiness D. Muscle weakness E.Ataxia F. GI Effects G. All the above H. A-E | H. A-E |
The use of parenteral Benzodizapines during the dental appointment reduces and alters what? | Anxiety and alters perception of time. |
What drug has a long half-life and metabolizes to an active metabolite to prolong its duration? | Diazepam |
What drug is metabolized primarily to inactivate metabolites? | Midazolam (Versed) |
This drug is found in Europe primarily but is sold into the US illegally and used inappropriately (been secretly given to women who were then ________). Fill in the blank. What am I? | Date Rape, Flunitrazepam (Rohypnol) |
Anterograde Amnesia produces what? | Amnesia at the beginning, when the drug is taken. |
What effect does Dizapam have on an outpatient dental procedure? | Respiratory depression |
Some cardiovascular effects may do what what a relief of anxiety occurs? | Fall in blood pressure and plus rate |
What visual effects are contraindicated and produced when taking Benzodiazepines? | Angle-closure (narrow-angle) glaucoma, diplopia ( single object viewed as two), nystagmus (rythmic oscillation of the eyeballs), and blurred vision. |
When taking Benzodiazapines, what are the common dental effects that are produced? | Xerostomia, increased salivation, swollen tongue, and a bitter metallic taste. |
Thrombophelbitis is what? | Extreme irritation of the veins |
Why may Parenteral Diazepam cause thrombophelbitis? | Propylene glycol is used to solubilize it. |
Benzodiazepines will interact in a "________" fashion with other CNS depressants. | additive |
T/F: Selective serotonin uptake inhibitors do not alter the clearance of diazepam. | False- they do alter the clearance of diazepam |
Levodopa's effectiveness is reduced by, A. Diazepam B. Levodopa C. Benzodiazepines D. Barbiturates | C. Benzodiazepines |
Barbiturates increase the effect of digoxin, phenytonin, and probenecide. Benzodiazepines are useful in short-term treatment of anxiety, panic attacks, insomnia, and alcohol withdrawal. A. both are true B. both are false C. first is false second is true | C. first is true second is false |
"_______" is used for acute treatment of seizures and conscious sedation as well as "_______" or during surgery. | Benzodiazepines and general anesthesia |
What are the manifestations of anxiety? | Restlessness, tension, tachycardia, and dyspena |
Medical uses for Benzodiazepine include what, A. anxiety control B. insomnia management C. treatment of epilepsy (seizures) D. all the above | D. all the above |
What are the two drugs of choice for an emergency situation in the treatment of epilepsy( seizures), A. digoxin B. diazepam C. probenecid D. lorazepam | B. diazepam and D. lorazepam |
What is the purpose of Benzodiazepines in combination (treatment) of alcohol? | Used to treat alcohol withdrawal syndrome |
What is the treatment to control muscle spasms (multiple sclerosis and cerebral palsy)? | Benzodiazepines |
What does orally administered diazepam do for dental procedures? | allay apprehension |
When is premedication used and why? | before surgical procedures to allay anxiety |
Conscious sedation with benzodiazepines is usually accompanied by what? | IV administration |
What two forms of amnesia can develop with conscious sedation accompanied by IV administration? | Anterograde amnesia and Retrograde amnesia |
What is it called when you forget the events after the injections? | Anterograde amnesia |
What is retrograde amnesia? | Take the pill and forget what has happened before you took the pill |
What type of benzodiazepines have been associated with respiratory depression and arrest when used for conscious sedation? | Parenteral Benzodiazepines |
What requires continuous monitoring of respiratory and cardiac functions and requires a dentist to have additional training? | conscious sedation |
What three benzodiazepines agents are most common according to Dr. Dawson in lecture? A. alprazolam (xanax) B. diazepam (valium) C. midazolam (versed) D. flurazepam (Dalmane) E. all the above | A-C |
"_______" are the original sedative-hypnotic agents? | barbiturates |
What is one noted good thing about barbiturates and one bad thing? | problems with their use are well documented and are associated with a high rate of abuse and complete cardiovascular and respiratory depression with an over-dose |
What drug has almost completely replaced the barbiturates for treating anxiety and insomia? A. methohexital B. secobarbital C. benzodiasepines D. amobarbital | C. benzodiazepines |
Barbiturates are still used at "_______" and to "_____,______,_______". | anticonvulsants, induce general anesthesia |
How are barbiturates absorbed and used? | orally and rectally; intravenously but not intramuscular |
IV agents that are inactivated by redistribution from site of action in the CNS, to muscles and adipose tissue. This belongs to what pharmacokinetics of barbiturates? | distribution |
"______" barbiturates are rapidly and almost completely metabolized by the liver. | Short and intermediate- acting |
Where are long-acting barbiturates excreted and how? | kidneys as a free drug |
How do barbiturates produce their effect? | Enhance GABA receptor binding and prolonging the opening of chloride channels |
Why may barbiturates act directly on chloride channels? | if you are given higher doses of barbiturates |
Mechanism of barbiturates may account for what? | ability to induce surgical anesthesia and pronounced generalized CNS depression effects. |
What is the main pharmacological effect of barbiturates? | CNS depression |
What occurs with a normal dose of barbiturates? | relaxation |
What occurs with an intermediate dose of barbiturates? | inhibitory fibers of the CNS are depressed, resulting in dis-inhibition and euphoria |
What occurs with a high dose of barbiturates? | hypnosis can be produced |
What occurs with the max dose of barbiturates? | anesthesia with respiratory and cardiovascular depression and finally arrest |
T/F: Barbiturates have a significant analgesic effect | F-they don't have a significant analgesic effect |
Barbiturates have an anti-convulsant action. Long-acting agents are used to treat epilepsy. A. both are true B. both are false C. first is true, second is false D. first is false, second is true | A. both are true |
Sedatives do not provide "_____". | analgesia |
When should these drugs never be administered unless it may benefit them more than it would be a risk? | pregnant women due to risking the fetus |
What may be attempted when taking sedative-hypnotic drugs? | suicide |
"_______" and "______" dependence has been observed with almost all drugs used to allay anxiety. | psychic and physical |
T/F: Depression caused by all sedative-hypnotics will add to depression caused by other CNS depressants. | True-an additive of depression does occur |
What are the uses for centrally acting muscle relaxants? | adjunct to rest and physical therapy for relief of muscle spasms associated with acute painful musculoskeletal conditions. May be used for symptomatic relief of TMJ disorder |
What drugs are examples of centrally acting skeletal muscle relaxants? | carisoprodol (Soma); chlorzoxazone (Parafon Forte DSC); methocarbamol (Robaxin); orphenadrine (Norflex); cyclobenzapine (Flexeril); diazepam (Valium) |
What does baclofen (Lioresal) do? | inhibits both monosynaptic and polysynaptic reflexes at the spinal level |
What is baclofen (Lioresal) indicated for? | spasticity from multiple scerosis or spinal cord injuries or diseases |
Both sedation and analgesia can be obtained from what? | opioid analgesics |
A nonopioid or an opioid can be used concomitantly with a sedative in what case? | when anxiety is an important component in pain relief |
What statements are special considerations to remember? | Pt.'s who are to use antianxiety agents should be driven to and from the dental appointment. Drugs are not a substitute for pt. management |
An indenofuran derivative is highly selective for what? | melatonin type 1 (MT1) and melatonin type 2 (MT2) receptors |
MT1 receptors may mediate phase-shifting effects of melatonin on a 24-hour biologic clock while MT 2 receptor regulates sleep: a. both are true b. both are false c. first is true, 2nd is false d. first is false, 2nd is true | both are false-MT1 receptors regulate sleep while MT2 receptors mediate phase-shifting effects of melatonin on a 24-hour biologic clock |
Centrally acting muscle relaxants do what? | exert their effects on the CNS to produce skeletal muscle relaxation |
What statements correlate with the pharmacologic effects of centrally acting muscle relaxants? | all CNS relaxants produce some degree of sedative effect because their action is on the CNS. The sedative effects dominate over the "selective" muscle-relaxant activity. Useful in treating uscle spasms and back and neck pain. |
What statement belong to the overview of centrally acting muscle relaxants? | exert their muscle-relaxing properties indirectly by producing CNS depression. Have no direct effect on striated muscle; do not directly relax tense skeletal muscles |
Zolpidem (ambien) has hypnotic and anxiolytic effects but what does the receptor specificity produce? | less muscle relaxant and anticonvulsant effects. |
What are likely to be useful in dentistry when an oral anxiolytic agent is desired for relaxing an anxious dentalpatient? | zolpidem (Ambien) |
T/F: Zolpidem (Ambien ) is a rapid-acting hypnotic that is less potent and has a shorter duration of action than buspirone (BuSpar). | F- Zaleplon (Sonata) is a rapid-action hypnotic that is less potent and has a shorter duration of action than zolpidem |
What drug appears to have a lower risk of next day risidual effects, even with use in middle of the night? | zaleplon (Sonata) |
This drug is known for anterograde amnesia, an unpleasant taste, and impaired driving the morning after nighttime administration | eszopiclone (Lunesta) |
What is an melatonin receptor agonist that has been approved for treatment of insomnia characterized by diffulculty falling asleep? | ramelteon (Rozeram) |
Whose mechanism of action is unknown and believed to be related to interactions with neurotransmitters in the CNS? | buspirone (BuSpar) |
Why are buspirone (BuSpar) anxioselective? | due to its selective anxiolytic action without hypnotic, anticonvulsant, or muscle-relaxant properties |
What do most pt.'s pefer? | Benzodiazepines |
What three drugs comprise a new class of drugs that are not benzodiasepines but appear to bind to benzodiazepine receptors and decrease sleep latency with little effect on sleep stages? | zolpidem, zaleplon, and eszopidone |
What drugs are all thought to have agonist effects on GABA? a. zolpidem b. buspirone (buspar) c. benzodiasepines d. zaleplon e. eszopidone f. all the above | all the above: zolpidem, buspirone (buspar), benzodiasepines, zaleplon, eszopidone |
T/F: zolpidem, zaleplon, and eszopidone are used to treat epilepsy only. | F-zolpidem, zaleplon, and eszopidone are used to treat insomnia only |
What is zolpidem (ambien) recently developed hypnotic used for? | short-term management of insomnia |
What are therapeutic uses determined by? | duration of action |
What type of barbiturates are used intravenously for induction of general anesthesia? | ultra-short acting barbiturates |
What type of barbiturates have little medical use and are replaced by benzodiasepines? | short- and intermediate-acting barbiturates |
Long-acting barbiturates are used for what? | treatment of epiepsy |
What is another name for the nonbenzodiazepine- nonbarbiturate sedative-hypnotics? | chloral hydrate (noctec) "mickey-finn" and buspirone (buspar) |
What statement belongs to chloral hydrate (noctec)? | an inexpensive, orally effective sedative-hypnotic drug with a rapid onset and short duration of action |
Therapeutic doses of chloral hydrate (norcet) do not produce what? | pronounced respiratory or cardiovascular depression |
What is used in dentistry for preoperative sedation for children and at what dose? | chloral hydrate (noctec); 50 mh/kg up to maximum of 1g |
T/F: a larger and larger dose must be used to produce an effect, and this dose can approximate the lethal dose | true-dose to produce an effect can result in the lethal dose |
What is porphyria? | a group of disorders involving heme biosynthesis |
Barbiturates are recommended with porphyria. They are recommended with intermittent or a positive family history of porphyria: a. both are true b. both are false c. 1st is true, 2nd is false d. 1st is false, 2nd is true | both are false- barbiturates contraindicated in both pt.'s with porphyria |
Why are barbiturates contraindicated in pt.'s with porphyria? | they stimulate an increase the synthesis of porphyrins which are already at an excessive level in this disease |
Barbiturates are simulators of what? | liver microsomal enzyme production |
What are liver microsomal enzymes responsible for metabolism? | many drugs |
an increase in the liver microsomal enzymes could do what? | Increase the rate of drug destruction and decrease duration of action |
With a usual dose barbiturates are relatively safe. CNS depression may be exaggerated in debilitated pt. or those with liver or kidney impairment: a. both are true b. both are false c. 1st is true 2nd is false d. first is false second is true | both are true |
what is an important fact with anesthetic dose? | with higher doses, concentrations in the blood can be lethal |
What statement does acute poisoning belong with? | lethal dose can only be approximated, severe poisoning will follow ingestion of 10x the hypnotic dose; life may be threatened when more than 15x the hypnotic dose is consumed |
chronic use of barbiturates can lead to what dependence? | physical and psycological |
how does an addict act over barbiturates? | progressively depressed and is unable to function |
T/F: tolerance develops to most effects and the lethal dose? | F- tolerance does develop to most effects but not to the lethal dose |