1. Basic Pharmacology
Block 2 Review

2. What are adrenergic agonist
Drugs that mimic the effects of adrenergic nerve stimulation (or stimulation of the adrenal medulla)
Mimic the effects of norepinephrine or epinephrine
These drugs are known as adrenomimetics or sympathomimetics
Remember the actions of the SNS are mediated through alpha and beta receptors.

3. Remember Alpha 1: most vascular smooth muscle, agonist contract
Beta 1: heart, agonist increase rate
Beta 2: respiratory and uterine smooth muscle, agonists relax.

4. Phenylephrine Methoxamine Clonidine methyldopa Dobutamine
Name alpha selective direct – acting agonists
Identify the major beta selective direct-acting agonist
Phenylephrine
Methoxamine
Clonidine
methyldopa
Dobutamine
Isoproterenol
Albuterol
Metaproterenol
Terbutaline

5. Epinephrine Norepinephrine dopamine Epinephrine Norepinephrine
List the major alpha and beta direct-acting agonists
Direct- acting agonists considered catecholamines
Epinephrine
Norepinephrine
dopamine
Epinephrine
Norepinephrine
Isoproterenol
Dopamine
dobutamine

6. Uses of this drugs Nasal decongestant ADHD CVS Ventricular Arthymias
Brochospasm
Shock

7. Organization of Class
The effect of the SNS can be blocked either by decreasing sympathetic outflow from the brain, suppressing release of NE from terminals or by blocking postsynaptic receptors.
Adrenergic antagonists reduce the effectiveness of sympathetic nerve stimulation and effects of exogenously applied agonists, such as isoproterenol.

8. ADRENERGIC BLOCKERS ALPHA BLOCKERS Alpha 1 Blockers Nonselective Alpha
Doxazosin Phenoxybenzamine
Prazosin Phentolamine
Terazosin
Most alpha antagonists allow vasodilatation and thus, decrease blood pressure( remember a-receptor activation results in vasoconstriction)

9. Non Selective Beta 1 selective Blockers Blockers
BETA BLOCKERS
Non Selective Beta 1 selective Blockers Blockers
Propranolol Metoprolol
Timolol Atenolol
Nadolol Esmolol
Acebutolol
Betaxolol
Labetalol - Both Alpha and Beta Blocker
Beta 1receptors found in the heart and their activation leads to an increase in HR and contractility .
Beta 2 receptor are found in SM of the respiratory tract, the uterus and blood vessels. Their activation leads to relaxation of SM

10. DRUGS AFFECTING NEUROTRANSMITTER UPTAKE OR RELEASE
Cocaine
Guanethidine
Reserpine

11. Main use
HTN
Benigh Prostate Hypertrophy
Angina
Glaucoma
Post MI

12. CNS 1 Drugs used to treat parkinsonism
Dopamine replacement therapy: levodopa and carbidopa
Dopamine Agonist Therapy: Bromocriptine.
Pergolide, pramipexole, ropinirole and rotigotine
Anticholinergic therapy:
Trihexyphenidyl
Benztropine
Biperiden

13. CNS 2 ANXIOLYTICS, HYPNOTICS AND SEDATIVES
Benzodiazepines- the most frequently used drugs for anxiety
Azaspirones- for example, buspirone
Carbamates- for example, meprobamate
Barbiturates- rarely used today because of severe side effects and a low therapeutic index. These drugs have generally been replaced by the benzodiazepines.

14. WHAT ARE THE THERAPEUTIC INDICATIONS FOR BENZODIAZEPINES
These drugs are used clinically as muscle relaxants and in the treatment of the following:
Anxiety disorders
Panic disorders- alprazolam is the drug of choice
Status epilepticus- diazepam is the drug of choice
Sleep disorders
Insomnia- all benzodiazepines can be sedating but lorazepam and temazepam are the most commonly used.
Alcohol withdrawal- Chlordiazepoxide most commonly used.

15. WHAT ARE THE THERAPEUTIC INDICATIONS FOR BARBITURATE ADMINISTRATION
Induction of anesthesia- thiopental
Anticonvulsants- e.g, phenobarbital
Treatment of anxiety
Induction of hypnosis
Why are benzodiazepines favored over barbiturates for the treatment of anxiety?
Benzodiazepines have a much higher therapeutic index than do barbiturates

16. CNS 3: CNS STIMULANTS 1. methyxanthines 2. amphetamine 3. nicotine
Main use: appetite control, ADHD, Narcolepsy, excitement and euphoric properties, decrease fatigue,

17. CNS 4: Antipsychotic Drug
Antipsychotic, also known as neuroleptics are drugs used primarily to treat psychotic states such as schizophrenia, delusional disorder and other hallucinatory states

18. TRADITIONAL ANTIPSYCHOTICS
PHENOTHIAZINES
EXAMPLES
CHLORPROMAZINE (THORAZINE)
FLUPHENAZINE (PROLIXIN)
THIORIDAZINE(MELLARIL)
PERPHENAZINE ( TRILAFON)
What distinctive side effects does thioridazine cause?
Pigmentary retinopathy
May cause cardiac arrhythmias and conduction block

19. Name a drug that belongs to this class Loxapine ( loxitane)
BUTYROPHENONES
Name two drugs in this class
Haloperidol ( haldol)
Droperidol( inapsine)
Haloperidol can also be used for
tourette’s syndrome
Huntington’s disease
Phencyclidine overdose- drug of choice
Side effects are Extrapyramidal side effects
DIBENZOXAZEPINES
Name a drug that belongs to this class
Loxapine ( loxitane)
THIOXANTHENES
Name a drug that belongs to this class?
Thiothixene ( navane)

20. CLINICAL USES AND SIDE EFFECTS
What are the clinical applications of traditional antipsychotic agents?
Treatment of agitated or psychotic state such as bipolar disease or schizophrenia. They are effective for positive symptoms of schizophrenia such as delusions, thought disorders and hallucinations.
Antiemetic therapy ( dopamine blockade except thioridazine )
Tourette’s syndrome: haloperidol
Intractable hiccups_ chlorpromazine
Antipruritic therapy_ promethazine ( histamine blockade)

21. Atypical antipsychotic drugs ( SEROTONIN-DOPAMINE ANTAGONISTS)
Examples
Clozapine ( clozaril)
Risperidone ( risperdal)
Olanzapine ( zyprexa)
This drugs are called atypical because in addition to blocking dopamine receptors they also produce significant blockade on serotonin
( 5-HT) receptors

22. CNS 5:ANESTHETICS * GENERAL * LOCAL
General anesthetics are given either as inhaled or intravenous agents.
They primarily have CNS effects
Local agents are injected at the operative site to block nerve conduction

23. INHALED AGENTS HALOTHANE ENFLURANE ISOFLURANE SEVOFLURANE
NITROUS OXIDE
There potency is defined base on the concept of minimum alveolar concentration ( MAC)

24. IV Thiopental Ketamin Propofol Etomidate fentanyl
Know their uses and side effect

25. ANESTHETICS COCAINE BENZOCAINE PROCAINE TETRACAINE LIDOCAINE
NAME THE ESTER ANESTHETICS
NAME THE AMIDE ANESTHETICS
COCAINE
BENZOCAINE
PROCAINE
TETRACAINE
LIDOCAINE
MEPIVACAINE
BUPIVACAINE
PRILOCAINE