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Pharmacology > Midterm Review... > Flashcards

Midterm Review... Flashcards

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1
Q

Routes of Drug Administration =

A

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)

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2
Q

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

A

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

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3
Q

Effects of pH on drug absorption?

A

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

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4
Q

Factors affecting drug absorption?

A

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

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5
Q

What are two phases of drug metabolism?

A

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.

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6
Q

What is efficacy and Potency?

A

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

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

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7
Q

Definitions of four types of drug interactions?

A
  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
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8
Q

Definitions for Tolerance, dependence & withdrawal:

A
  • 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
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9
Q

Activation of muscarinic receptors (ANS) on different organs:

A
  • 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
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10
Q

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

A

Pilocarpine is used for Glaucoma - (Cholinergic Agonist)

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

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11
Q

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

A

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

Used for - MG & Alzheimers

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12
Q

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

A

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

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13
Q

What are the effects & side effects of cholinergic antagonists?

A

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

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14
Q

Classification of Cholinergic Antagonists:

  1. Atropine
  2. Scopolamine
  3. Ipratropium
  4. Dicyclomine
  5. Succinylcholine
A
  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
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15
Q

Effects of stimulations of a1 adrenoceptors:

A
  • a1 = cause constriction of muscle = BLOCKER - Vasoconstriction, Increase BP, Increase peripheral resistence, Mydriasis, Increased CLOSURE of internal sphincter of Bladder
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16
Q

Effects of stimulations of a2 adrenoreceptors

A
  • a2 = Agonists - down-regulates - used in systemic HYP, cause feedback inhibition
  • Inhibition of norepinephrine release, Inhibition of Acetylcholine release, Inhibition of Insulin release
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17
Q

Effects of stimulations of ß1 & ß2 adrenoreceptors

A
  • 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
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18
Q

Uses for:

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

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.
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19
Q

Drugs used for BPH & Pheochromocytoma?

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A
  • 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
20
Q

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

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A

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.

21
Q

Example & uses of selective ß-blockers:

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A

Metoprolol - HYP, Myocardial, Infection, Angina Pectoris

  • Atenolol
  • Bisoprolol
  • Esmolol
  • Betaxolol
  • Acebutolol
22
Q

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

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A

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

23
Q

Effects of botulinum toxin & spider venom on Acetylcholine?

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A

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

24
Q

Effects of Reserpine, Cocaine & Imipramine on norepinephrine?

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A

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

25
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
26
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.
27
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.
28
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.
29
Therapeutic uses of Lidocaine?
Used for IV for Tx. of cardiac Arrythmia, also an *Amides* type of local anasthetic
30
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).
31
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
32
\_\_\_\_\_\_\_\_\_ 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.
33
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.
34
What are the uses for typical neuroleptics Chlorpromazine & Haloperidol?
* **_Chlorpromazine_** - Parkinsonism, Nausea, vomiting & hiccoughs. * **_Haloperidol_** - Tourett's Syndrome, Huntingtons disease, Parkinsonism.
35
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.
36
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)
37
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.
38
Naloxone (given for Opioid poisoning/overdose) & Naltrexone/ReVia are both categprized as Opioid \_\_\_\_\_\_\_\_
Opioid Antagonists
39
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.
40
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
41
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
42
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)
43
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)
44
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.
45
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.
46
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.
47
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_**

Pharmacology (4 decks)

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