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What are seditives commonly used for? What are the 3 major types SPF anxiety?
- To reduce anxiety induce sleep.
- 1. Anxiety attacks
- 2. Situational anxiety
- 3. Generalized anxiety disorder
List three families of sedatives.
- 1. GHB (gamma hydroxybutyric acid)
- 2. Barbiturates
- 3. Benzodiazepines
Explain the chemical nature of how sedatives work.
they activate chloride ion channel in neural membranes by activating GABA Receptors. When GABA binds It opens a specific ion channel allowing more chloride into the cell. This increase negative potential in the cell causing hyper polarization inhibiting post neuron firing.
What stimulation causes reduction in anxiety?
GABA stimulation in limbic System.
Stimulation that promotes sleep.
GABA stimulation in cortical areas
Stimulation inducing amnesia
GABA stimulation in hippocampus and cerebral cortex
what determines if a sedative induces sleep or relieves anxiety?
Dosage. Low dose = anxiety
What does GHB stand for?
Gamma hydroxybutyric acacid trade name xyrem
what is GHB used for?
Legally prescribed for sedation in large doses. Commonly used as illegal date rape.
Why are barbiturates not commonly used?
Low therapeutic index with side effects of respiratory depression and high physical dependence.
How did barbiturates work?
Directly stimulating inhibitory gaba type chloride channels as well as inhibiting types of stimulatory receptors. This leads to reduction of CNS activity
Name three barbiturates.
- 1- phenobarbital
- 2- sodium Pentothal (thiopental)
- 3- fiorinal or fiorcet
What barbiturate is used to tx seizures?
What barbiturate is used for induction of anesthesia ?
Sodium Pentothal (thiopental )
What barbiturates are used for tension head aches and migranes?
Fiorinal and fioricet
What are two major adverse effects of barbiturates?
- - respiratory depression
- - physical dependence
How do benzodiazepines work?
By potentiating effect of naturally occurring gaba but is limited by naturally occurring gaba.
true or false: benzodiazepines are lipophobic.
FalseFalsies!! Lipophilic :)
What do benzodiazepines treat?
Anxiety, insomnia, delirium tremens, status epilepticus and amnesia.
What are some adverse effects of benzodiazepines?
- - psychological dependence
- - amnesia
- - sudden withdrawal will have serious effects
Name three benzodiazepines with a brief explanation.
- alprazolam (xanax): tx anxiety and panic attacks
- lorazepam (ativan): most commonly used. tx anxiety and withdrawal symptoms from alcoholics
-Diazepam (valium): occasionally used for anxiety before sx or dental procedures, muscle spasticity, status epilepticus.
what are some clinical symptoms of parkinson's disease?
produces movement disorders called dyskinesias.
this includes tremors, rigidity, bradykinesia, disturbed posture, and akinesia. Leads to psychological disturbances.
Give a chemical explanation of Parkinson's.
Due to lack of dopamine in striatum of brain. Balance must be maintained between Dopamine and aceytlecholine.
what produces dopamine?
substantia nigra cells in the striatum.
What are two possible unique situations causing parkinson's?
- 1. contamination of methyl fentanyl (heroin like street drug)
- 2. cycad seed flour, eaten in guam, containing brain neurotoxin.
Why cant dopamine be given orally?
- It will be metabolized quickly.
- It will not cross the BBB.
- It will cause other undesired effects.
What are three treatment methods of Parkinson's?
- 1. give a dopamine precursor
- 2. give a dopamine analog agonist
- 3. inhibit rate of dopamine metabolism.
Name a dopamine precursor.
Levodopa, or L-DOPA
How does L-DOPA become Dopamine?
It is converted by an enzyme called DOPA decarboxylase
How must L-DOPA (if given alone) be given and why is this negative?
It must be given in high doses. This high dose causes increased heart rate and blood pressure.
What is carbidopa?
Carbidopa is an inhibitor of DOPA decarboxylase that does not cross the BBB which when combined with L-DOPA allows L-DOPA to reach the brain before being converted to Dopamine.
What is the most common dopamine precursor?
What are L-DOPA/carbidopa's side effects?
- 1. GI disturbances
- 2. orthostatic hypotension
- 3. movement disorders
- 4. on-off efficacy
- 5. tachycardia due to B1 stimulation
- 6. aggravation of adverse anti-psychotic drugs
what is a downfall of L-DOPA?
efficacy does not last indefinitely.
Name three dopamine agonists.
- 1- pramipexole (mirapex)
- 2- ropinrole (Requip)
- 3- Bromocriptine (Parlodel)
What are dopamine agonists?
molecules which imitate the action of dopamine. must be able to cross BBB.
Name the generic name and adverse effects for Mirapex
- somnolence, sudden sleep attacks
Give the generic name and adverse effects for Requip
- dizziness, somnolence, sudden sleep attacks, nausea
What are two drugs approved for RLS?
Mirapex and Requip
Give generic and common use for Parlodel.
- used to dry up mothers milk when ready to stop breastfeeding.
Name an inhibitor of dopamine metabolism.
Selegiline (Eldepryl, Deprenyl)
How does Selegiline work?
inhibitor of type B monoamine oxidase which metabolizes dopamine. This produces a higher dopamine level.
What is selegiline usually paired with?
The patch Emsam uses what drug and treats this...
under category of selegiline and tx's depression
How does Amantadine (Symmetrel) work?
Promotes release of dopamine from striatum. only works for a month or two. Formly used to reduce flu symptoms. Off-label use of fatigue associated with MS
Give three non-pharmacological treatments of Parkinson's.
- 1- Transplants of stem cells
- 2- posteroventral medial pallidotomy
- 3- Electrical stimulation of subthalamic nucleus.
Describe Albuterol (ProAir, Proventil HFA).
- -most commonly used B2 agonist.
- - used to stop asthma attack
- - administered with MDI
Combo of Atrovent and albuterol. Used for COPD
Describe Salmeterol (Serevent).
- -Newer long acting B2 agonist.
- -12 hour half-life.
- - prophylactic use.
- - usually combined with fluticazone.
Name four steroids for asthma.
- 1- Fluticazone (Flovent)
- 2- Triamcinolone (Azmacort)
- 3- Mometasone (Nasonex nasal inhaler)
- 4- Advair
How do steroids work for treatment of asthma?
They are inhaled and inhibit influx of inflammatory cells, block synthesis of prostaglandins, and reduce formation of inflammatory cytokines.
What is the primary choice asthma drug?
steroid combined with B2 agonist.
Give some positives and negatives of taking steroids by inhaler.
- -reduces systemic steroid effects (weight gain, water retention, HTN)
- -sore throat/ oral infection
- -Candida Albicans
Give generic and main use of Flovent.
- Steroid used for asthma. Rapid onset. Used for nasal allergies and possible to stop asthma attack (when combined with albuterol).
Give generic and main use for Nasonex nasal inhaler).
- Anti-inflammatory steroid. Used DPI for astma and nasal allergies. Also available in cream for eczema.
What is Advair made of?
Long acting combo of Flovent and Serevent
(steroid and B2 agonist)
What is Symbicort?
New combo of budesonide and formoterol fumarate.
Name four non-steroidal asthma drugs.
- 1- Antileukotriene agents: montelukast (Singulair)
- 2- Theophylline (Theo-Dur, Slo-Bid)
- 3- Aminophylline
- 4- Cromolyn Sodium (Intal)
What drug is an Antileukotriene agent?
What does montelukast (Singulair) inhibit?
synthesis of leukotriene D4
What is Theophylline (Theo-Dur) used for?
prophylactic drug for asthma. Narrow TI. Relative to caffeine.
What is Aminophylline used for and how is it administered?
in ionic form given IV. For acute asthma attacks.
also marketed to remove cellulite.
How does Cromolyn sodium work and what is it for?
prophylactic Tx of asthma.
Stabilizes membrane of mast cells to prevent release of histamine.
Name two Alpha 1 antagonists.
What are the effects of Flomax and Cardura?
- -cause peripheral vasodilation
- -main tx of BPH (Benign prostate hypertrophy).
What drugs are used for Benign Prostate Hypertrophy?
Flomax and Cardura
What are three adverse effects of BPH drugs?
- 1- orthostatic hypotension
- 2- nasal congestion
- 3- inability to ejaculate
Name a Non Specific alpha 1 and Beta blocker:
What does Coreg (carvedilol) help treat?
- -causes peripheral vasodilation and slowing of heart rate.
- - used with CHF and atrial fibrillatrions
When can the use of Coreg (carvedilol) be dangerous?
When used by asthmatics or pts with respiratory difficulties. it will block response to beta-2 agonists
Name a non-specific B Blocker.
- Propranolol (Inderal).
- -clinical use of B1 blockade.
- -decreases intensity and heart rate contraction
*may cause bronchoconstriction in susceptible individuals*
Name 6 possible clinical uses of Propranolol.
- 1- tx of hypertension
- 2- tx of angina
- 3- tx of cardiac tachycardias
- 4- prophylactic tx of stage fright (off label)
- 5- proph. use of migraine prevention
- 6- reduction of tissue damage after MI
Name three Specific B1 Blockers.
- 1- Metoprolol (Lopressor)
- 2- Atenolol (Tenormin)
- 3- Nevibolol (Bystolic)
When are metoprolol and atenolol used?
- - most commonly for anti HTN drug
- - taken with ACE inhibitors to lower post-MI mortality
What is a long term adverse affect of atenolol?
increased risk of type 2 diabetes.
Name a few of the adverse effects of Metoprolol and Atenolol.
- 1. increased risk of heart block
- 2. prevention of tachycardia
- 3. tiredness/ lethargy
- 4. nightmares
- 5. rebound tachycardia.
How does Nevibolol (Bystolic) work?
specific beta blocker that causes vasodilation by stimulating nitric oxide release.
What two drugs are used for tx of glaucoma?
1- Timolol (Timoptic) Blocks B1 and B2 receptors in eye
2- Betalol (Betoptic) acts on B1.
Name three Anti-Adrenergic drugs acting on CNS.
- 1. Reserpine
- 2. Clonidine (Catapres)
- 3. Cyclobenzaprine (Flexeril)
Is Reserpine still commonly used?
No! caused major depression
How does Clonidine work?
blocks receptors in CNS inhibiting SNS (decreasing HR)
What is another use of Clonidine?
Tx of HTN (7 day transdermal patch)
Reduction of sympathetic stimulation in alcohol withdrawal and with tx of ADHD. Usually combined with Ativan or Librium.
What is Cyclobenzaprine (Flexeril) used for?
Tx of muscle spasm's.
Explain two general mechanisms of action in muscle meds.
- 1- non-depol. blockers bind to acetylcholine
- 2- depol blockers bind to ACh receptor
Name a depolarizing neuro muscular blocker.
What is the primary use of Succinylcholine and how can it be dangerous?
- - muscle spasms.
- fast metabolism
- -can kill people w/ malignant hyperthermia
Name four non-depolarizing neuro-muscular blockers.
1- Zemuron- short half life
2- Panulon- intermediate half life
3- Norcuron- intermediate acting
4- Tubocurarine- original neruomus. blocker used on arrow tips. long half life.
name sympathetic effects of nicotine.
increased hr and vasoconstriction
name parasympathetic results of nicotine
increased salivation and GI motility
How is nicotine used with insects?
High doses can cause overload of conflicting signals producing death.
What is the primary use of nicotine?
Name the nicotine gum
Give three nicotine patches.
- - Prostep
- - Nicoderm
How is habitrols delivery of nicotine different than prostep and nicoderm?
habitrol is much slower delivery
what is the % of nicotine patch success?
What is Varenicline (Chantix) and what is it used for?
- - Partial nicotine agonist
- -similar effects to nicotine, helpful for quitting smoking.
What negative effect has been publicized about Chantix?
Give an example of a non-western nicotine like drug.
- betel palm seed wrapped in leaf of betel pepper.