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Routes of Drug Administration =

Enternal -

  1. Oral (most common, convenient, DELAYED action, C/I Vomiting)
  2. Sublingual - QUICK in action
  3. Rectal

Parental - 

  1. IV
  2. IM
  3. SC

Others - include inhalation, Intranasal, Intrathecal, Topical, Transdermal & (Intradermal - PPD test or allergy test)


What is First Pass effect? What forms of administration surpass this effect and go straight to systemic circulation?

Liver metabolism prior to reaching the systemic circulation. IV, IM and sublingual go straight to systemic. 

* Drugs cross membranes by passive diffusion or active transport


Effects of pH on drug absorption?

Acidic drugs aka H+ & A- are absorbed better in ST

Basic drugs aka B & H+ are absorbed better in SI which has higher pH


*drug passes more readily if uncharged


Factors affecting drug absorption? 

Physical - blood flow, surface area, movement time

more blood flow = more absorbpton

more surface area = more efficient absorption

quick mmt thru GI = less absorption

Drug -factors - ionization, molecular weight, solubility, formulation

Patient factors - pressence of food in GI, ST acidity & blood flow to GI tract


What are two phases of drug metabolism?

Phase 1 = Cytochrome P450 system of enzymes in SER oxidizes or reduces to more polar form.

Phase 2 = Polar group like glutathione is conjugated to the drug increasing polarity. 


What is efficacy and Potency?

Efficacy = degree to which a drug is able to induce maximal effects

Potency = amount of drug required to produce 50% of the maximal response


Definitions of four types of drug interactions? 

  1. Addition - equal to combined response 1+1 = 2
  2. Synergism - response is greater than 1+1 = 3
  3. Potentiation - no effect drug enhances effect of 2nd drug 0+1 = 2
  4. Antagonism - drug inhibits 1+1 = 0


Definitions for Tolerance, dependence & withdrawal:

  • Tolerance - decrease response to a drug over time - will not produce same action eventually
  • Dependence - need drug to Fx. normally, drug cessation produces withdrawal symptoms
  • Withdrawal - drug is no longer administered to a dependent patient


Activation of muscarinic receptors (ANS) on different organs:

  • Eye - constrict pupil
  • Cardiovascular - lowers HR
  • Resp. - Bronchial constriction & increase fluids
  • GI - Increase motility - relax sphincters
  • GenitoU - Relax sphincters & bladder wall contract
  • Glands - Increased secretions


What is the use for Pilocarpine? Donezepil? What type of Cholinergic drugs are they?

Pilocarpine is used for Glaucoma - (Cholinergic Agonist)

Donezepil is used for Alzheimer's - (Indirect-acting on prolonging the life of Acetycholine) - Inhibit - aka Anticholinesterases


What are the actions of Indirect-acting Cholinergic agonists aka Anticholinesterases? What conditions are they used for?

They inhibit enzymes (AChE) which terminates the action of Acyteylcholine thus prolonging the lifetime of Acetylcholine.

Used for  - MG & Alzheimers


What two drugs are used in the treatment of Organophosphate poisoning?

Pralidoxime (hydrolyze phosphate bond &reactivate enzyme) & Atropine (blocks effects of excess Acetylcholine)


What are the effects & side effects of cholinergic antagonists? 

Antagonize the effect of Acetylcholine. Block muscarinic receptors of Parasympathetic nerves or nicontinc receptors blockers by blocking skeletal muscle reactions and relaxing them. 

Side effects = dry mouth, dry eyes, blurred vision, constipation, & urinary retention


Classification of Cholinergic Antagonists:

  1. Atropine
  2. Scopolamine
  3. Ipratropium
  4. Dicyclomine
  5. Succinylcholine 

  1. Atropine - prevent resp. secretions - Parkinsonism, Severe Bradycardia, Enuresis (Muscarinic Antagonists) 
  2. Scopolamine - prevent motion sickness - transdermal patch (Muscarinic Antagonists) 
  3. Ipratropium - COPD - produce bronchodilation NOT good for ASTHMA patients  (Muscarinic Antagonists) 
  4. Dicyclomine - IBS
  5. Succinylcholine - ideal for intubation, rapid & short duration (Nicotinic receptor/blocker) - skeletal muscle relaxation


Effects of stimulations of a1 adrenoceptors:

  • a1 = cause constriction of muscle = BLOCKER -  Vasoconstriction, Increase BP, Increase peripheral resistence, Mydriasis, Increased CLOSURE of internal sphincter of Bladder 


Effects of stimulations of a2 adrenoreceptors 

  • a2 = Agonists - down-regulates - used in systemic HYP, cause feedback inhibition
  • Inhibition of norepinephrine release, Inhibition of Acetylcholine release, Inhibition of Insulin release


Effects of stimulations of ß1 & ß2 adrenoreceptors 

  • ß1 = BLOCKER - can block actions of ß2 - affinity to epinephrine & norepinephrine
  1. Tachycardia, Increased Lipolysis, Increased Myocardial contractility, Increased release of RENIN
  • ß2 = Agonist - higher affinity for epinephrine - used for ASTHMA
  1. Vasodilation, Sl. decreased peripheral resistence, Bronchodilation (ASTHMA), Increased muscle & LV glycogenolysis, Increase release of GLUCAGON, Relaxed Uterine smooth muscle


Uses for: 

  1. Epinephrine
  2. Dobutamine
  3. Albuterol
  4. Methylphenidate

Catecholemines - Direct Acting Adrenergic Agonist

  1. Epinephrine - intense asthma, anaphylactic shock
  2. Dobutamine - Stimulate Heart

Noncatecholermine - "      "

  1. Albuterol - Bronchodilator

Indirect acting Adrenergic Agonist

  1. Methylphenidate - aka Ritalin - ADHD, Narcolepsy, appetite control - CNS stim.


Drugs used for BPH & Pheochromocytoma?

  • BPH - Alfuzosin/Uroxatral, decrease BP, relax smooth muscle in UB neck & prostate.
  • Pheochromocytoma (tumor of adrenal medulla) - a1 & a2 blockers used - cause vasodilation and lower BP - treat hypertensive episodes, Phentolamine/Regitine & Phenoxybenzamine  



Use & C/I's of non-selective ß-blocker:

All used in HYP. B-blockers will prevent the actions of B2. aka decreased Glucagon & Glycogenolysis. Caution of Propranolol with Diabetes patients - - Hypoglycemia may occur after Insulin injection.


Example & uses of selective ß-blockers:

Metoprolol - HYP, Myocardial, Infection, Angina Pectoris

  • Atenolol
  • Bisoprolol
  • Esmolol
  • Betaxolol
  • Acebutolol


Example & advantage of using mixed a & ß blockers in the treatment of HYP: 

Labetalol & Carvedilol - both decrease BP w/o causing reflex Tachycardia.


Effects of botulinum toxin & spider venom on Acetylcholine?

effectively weaken a muscle for a period of three to four months


Effects of Reserpine, Cocaine & Imipramine on norepinephrine?

Inhibit transport of norepinephrine from the cytoplasm into presynaptic vesicles. Causes ultimate depletion of Norepinephrine. Used in HYP


MOA of:

  1. Carbidopa
  2. Selegiline
  3. Bromocryptine
  4. Amantidine 


All used in treatment of Parkinsons - 1-3 are DOPAMINE Replacement therapy (DRT) & 4 is a Dopamine receptor agonist therapy (DRAT)

  1. Carbidopa - (DRT) diminishes L-Dopa in peripheral tissues

  2. Selegiline - aka Deprenyl (DRT) - inhibitor of monoamine axidase-B (MAO-B), enzym that metabolizes dopamine in CNS.

  3. Amantidine - (DRT) antiviral for Influenza as well, enhances synthesis from neurons. 

  4. Bromocryptine - (DRAT) - Powerful dopamine-receptor agonist, excitation in basal ganglia


What are some withdrawal symptoms for Benzidiazepines? What are MOA for Benzodiazepines & Barbiturates? 


Barbiturates - enhance Fx. of GABA in CNS enhancing duration of CHLORIDE channel openings.  produce sedation in low doses and hypnosis, coma or death in high doses. Withdrawal includes anxiety, nausea, vomiting, HYPOtension, seizures and psychosis. 

Benzodiazepines - most widely used anxiolytic drugs - Inhibitors. bind to GABA receptors enhancing affinity - more frequent openings of CHLORIDE channels.

Withdrawal appears as confusion, anxiety, agitation & restlessness. Shorter half-lives will induce more abrupt & severe withdrawal. 


Uses and types for:

  1. Diazepam
  2. Alprazolam
  3. Flumazenil
  4. Bupropion

  1. Diazepam - long-lasting - Valium - Anxiety, Skeletal spasms, spasticity in MS, cerebral palsy - poisoning common

  2. Alprazolam - Shorter acting - Xanax - antidepressant, anxiolytic & panic attacks

  3. Flumazenil - benzodiazepines receptor antagonist - used to reverse sedative effects after anesthesia or overdose w. benzo's.

  4. Bupropion - Psychomotor (CNS) stimulant - antidepressant, can reduce cigarette cravings.


MOA of local anesthetics. Effects of Epinephrine when used with local anesthetics? 

Block the SODIUM channels in the nerve mebrane - no generation of action potential. Epinephrine may be mixed with certain local anesthetics in order to retard their systemic absorption. Causes Vasoconstriction. 

Effect order is pain fibers => sensory fibers => motor fibers. 


Therapeutic uses of Lidocaine? 

Used for IV for Tx. of cardiac Arrythmia, also an Amides type of local anasthetic


Classification of antidepressant drugs. Which group is most widely used? 

Increase concentration of norepinephrine or serotonin in synaptic cleft.  Inhibit reuptake of neurotransmitters. Take 2-3 weeks to work. 

Two types: 

  1. SSRI's - Selective Serotonin Re-Uptake Inhibitors - most widely used - inhibit reuptake of serotonin (Min. side affects) -also used for eating D/O's, panic D/O's, OCD, borderline personality D/O's. (FLUOXETINE/Prozac - increased suicide rate) ........................................................................................
  2. TCA's - Tricyclic Antidepressants - block reuptake of biogenic amines including norepinephrine & serotonin, lots of side effects, three-ring core structure. Also used in enuresis, chronic pain, neuralgia, migraine, agoraphobia w. panic attacks, Obsessive Cumpulsive Neurosis (Clomipramine/Anafranil). 


Cheese, beer & red wine are all rich in ________ and should not be eaten when taking MAO inhibitors. Which Atypical antidepressant is known to cause priapism in males? 

  • Tyramine - (can cause hypertensive crisis)
  • Trazodone/Deyrel


_________ is a standard drug used in bipolar treatment D/O's. Why are serum levels routinely checked in patients taking this? 

  • Lithium
  • Associated with hypothyroidism (gland grows) & Nephrogenic Diabetes Insipidus (KD's no longer respond to action of ADH) - both are reversible once lithium use is stopped. 


Classification of Neuroleptics: What are some extrapyramidal effects? 

  • Block Dopamine (increasing Prolactin release), muscarinic cholinergic, a-adrenergic & H-1 histaminergic receptors. - Produces antipsychotic effect.  Used in Tourette's, Huntington's, Counterflow & Parkinsonism tremors, rigidity & shuffling gate & neuroleptic malignant sysndrome. 
  • Extrapyramidal effect in basal ganglia - Dystonia (spasms of face), Akathisia (motor resltessness), tardive dyskinisia (lip smacking) & parkinsonism. 


What are the uses for typical neuroleptics Chlorpromazine & Haloperidol?

  • Chlorpromazine - Parkinsonism, Nausea, vomiting & hiccoughs.
  • Haloperidol - Tourett's Syndrome, Huntingtons disease, Parkinsonism.


Actions & advantages for using atypical antipsychotics? Side effects & precautions while using Clozapine?

  1. These drugs reduce both negative & positive symptoms of schizophrenia, while causing a minimum of extrapyramidal side effects.
  2. Positive = halucinations, delusions, D/O'd thought, agitation & Negative = withdrawal, flat affect, anhedonia) 
  3. Clozapine/Clozaril - can cause severe agranulocytosis, shd check WBC count on weekly basis. More prone to infections.


What are some causes for Neuroleptic Malignant Syndrome? Symptoms, treatment? 

  • Causes: side effect of antipsychotic drugs/neuroleptics. 
  • Symptoms: Catatonia, Rigidity, Stupor, Fluctuating BP, fever & Dysarthria
  • Treatment: Need to increase Dopamine Action, with Bromocryptine (Dopamine agonist) or Dantrolene (muscle relaxant) 



Definition & classification of narcotics. Danger of using mixed group while withdrawing from a strong agonist? 

Class 1 - act on receptors in CNS to reduce perception to pain. Mu (µ), Kappa (k) & delta (d) receptors - most actions of narcotic analgesics are mediated by Mu receptors.

  • Using mixed agonist will give results similar to morphine. They are agonists of kappa but antagonists of Mu, result like methadone. 



Naloxone (given for Opioid poisoning/overdose) & Naltrexone/ReVia are both categprized as Opioid ________

Opioid Antagonists


Actions of Morphine on:

  1. CNS
  2. Eye
  3. Respiration
  4. Cardiovascular
  5. GI & GU systems

What are some withdrawal symptoms of narcotics? 

  1. CNS - drowsiness & sedation, reduction of awareness of pain, nausea in ambulatory pt's. Effective cough suppressant (medulla)

  2. Eye - pupillary constriction - pinpoint pupil

  3. Respiration - depression - direct action on CNS

  4. Cardiovascular - no effect

  5. GI & GU systems - spasm, constipation, urinary retention 

  • Withdrawal Symptoms include: autonomic hyperactivity, Diarrhea, vomiting, chills, fever, tearing, runny nose, tremors, ABD cramps & severe pain. 


MOA & adverse effect of Phenytoin?

Phenytoin - Antiepileptic Drug - blocks voltage gated sodium channels by selectively binding to channel. 

  • Adverse effects are Gingival Hypertrophy & megaloblastic anemia


Drugs of choice for which conditions? (Generalized Epilepsy)

  1. Phenytoin, Carbamazepine, Phenobarbital, Primidone, Valporic Acid
  2. Ethsuximide 
  3. Valproic Acid
  4. Diazepam 
  5. Phenytoin, Diazepam

  1. tonic-clonic - Phenytoin, Carbamazepine, Phenobarbital, Primidone, Valporic Acid

  2. abscence - Ethsuximide 

  3. myoclonic - Valproic Acid

  4. febrile seizures - Diazepam

  5. status epilepticus- Phenytoin, Diazepam

Inhibit sodium into Neuron; block sodium channels to block excitation


What is the MOA of H2-receptor antagonist on GI tract? Examples? 

  • Prevent histamine-induced acid release
  • Cimetidine (inhibits CP-450), Ranitidine (less inhibition of CP-450) & Famotidine (No inhibition of CP-450) and Nizatidine (Axid)


What is the MOA of Proton pump inhibitors on GI tract? Examples? 

  • Inhibit H+-K+ - ATPase enzyme of parietal cell supressing secretion of hydrogen ions into gastric lumen. Reduces acid production & helps in healing peptic ulcers, used to treat GERD, Duodenal ulcers & hypersecretory states (Zollinger Ellison syndrome).
  • Examples: Omeprazole (Prilosec), Lansoprazole (Prevacid), Esomeprazole (Nexium), Pantoprazole (Protonix), Rabeprazole (Aciphex)


What is the use of Misoprostol on GI tract? What is its important adverse effect? 

  • Misoprostol - (Prostaglandins) - Increase HCO3 & mucin release. Reduces acid secretion & prevention of ulcers in aspirin & NSAIDS users.


What are mechanisms of antidiarrheal actions of Diphenoxylate with atropine? And of Bismuth Subsalicylate?

  • Antimotility agents - Diphenoxylate is an agonist at opiate recptors in GI tract & Atropine is anticholinergic & blocks muscarinic receptors. Both inhibit peristalsis and indicated by Diarrhea.
  • Bismuth Subsalicylate is an absorbent - (Pepto-bismol) - works by decreasing flow of fluids & electrolytes into bowel, reduces inflamm. in intestines & may kill organisms that cause diarrhea. 


These are important drugs used in treatment of ______ _______ & ________ disease? 

  1. Mesalamine
  2. Olsalazine
  3. Balsalazine
  4. Sulfasalazine
  5. Infliximab

Ulcerative Cholitis & Crohn's disease drugs. Infliximab is best drug for Crohn's - it inhibits TNF-a (proinflammatory protein), also used for Rheumatoid arthritis.


These are some names of important _____ _____ and cathartics:​

  1. Bisacodyl - increase intestinal motility
  2. Cascara
  3. Senna
  4. Phenolphthalein (Ex Lax) 


stimulant laxatives and cathartics