Pharmacology Board Exam Review Video Notes

Drug Names:

  • Chemical name-determined by the chemical structure of the compound; the code name

  • Trade (Brand) name-Motrin, Advil (uppercase)

  • Generic name-ibuprofen (lowercase); before marketing (official name)

Characterization of Drug Action:

  1. Potency

  • function/the amt of the drug requires to produce an effect

  • less amt=more potent

  • review proper dose of each drug before it’s prescribed

  1. Efficacy

  • the maximum intensity of effect or response that can be produced by a drug

  • giving more drug won’t increase it, but increase the probability of an adverse reaction

  1. NOT related

Pharmacokinetics: the study of how a drug enters the body, circulates within, and changed, and leaves

  1. Four Major Steps: ADME

  • absorption

  • distribution

  • metabolism (biotransformation)-primary organ involved is the LIVER

  • excretion

Half-life: amt of time that passes for its [ ] to fall to half of its original blood level

  • 4-5 half lives for a drug to be considered eliminated from the body

  • few drugs show zero-order kinetics (rate of metabolism remains constant over time)

Routes of Administration Dose Forms:

Onset-time it takes for the drug to begin to have its effect

Duration-the length of time of a drug’s effect

Enteral-via GI tract (oral, sublingual, rectal)

  1. Oral

  • Pros-small intestine presents large absorbing area, produces slower onset of action

  • Cons-nausea, vomiting, some drug inactivated by acidity or enzymes, drug interactions, pt cooperation

  1. Rectal

  • Pros-for vomiting or unconscious, local or systemic effect

  • Cons-poorly and irregularly absorbed, poor pt acceptance

Parental-via outside GI tract (intravenous)

  1. Injection

IV

  • Pros-most rapid drug response, predictable response, emergencies

  • Cons-phlebitis, drug irretrievability, allergy, side effects related to high plasma [ ]

Intramuscular

  • Pros-increased tolerance to irritating drugs, allows injection suspensions (sustained effect)

Subcutaneous (insulin)

  • Cons-irritating solutions may cause sterile abscesses

  1. Inhalation

  • Pros-rapid onset of action, no needles

  • Cons-popular route for abuse of drugs

  1. Topical

  • Pros-systemic side effects are rare

  • Cons-increased risk of systemic side effects if surfaces are large and/or abraded, inflamed, or sloughing; intraorally spayed anesthetics may be absorbed into blood stream

Other

  • Intradermal-epidermis of skin

  • Intrathecal-spinal subarachnoid space

  • Intraperitoneal-body cavity

Agonists and Antagonists:

  1. Agonist

  • affinity for a receptor

  • combines with the receptor

  • produces effect

  1. Antagonist

  • counteracts action of agonist

  • Ex) competitive, noncompetitive, physiologic

Drug Tolerance:

Therapeutic Index= LD50/ED50

  • If small=toxicity is more likely

Pharmacologic Effects of Cholinergic Agents and Anticholinergic Agents

  1. Cholinergic (Parasympathetic/cholinergic) ; acetylcholine

  • increase saliva, decrease HR + BP, pupil constriction

  1. Anticholinergic (Mimic sympathetic/adrenergic) ; epinephrine

  • decrease saliva, increase HR + BP

Drug used to treat xerostomia

  • Pilocarpine-Salagren; parasympathetic/cholinergic

Hypertension Drugs: ABCD

  1. Angiotensin Converting Enzyme (ACE) inhibitors

  • inhibit the enzyme that produces angiotensin II, which narrows blood vessels

  • dry cough

  • Drugs: enalaPRIL, lisinopRIL, PRIL

  1. Angiotensin II Receptor Blockers (ARB)

  • block action of angiotensin II (narrows blood vessels)

  • Drugs: losarTAN, TAN

  1. Beta blockers

  • Beta 1=increase heart muscle contraction

  • Beta 2=relax bronchial smooth muscles

  • Drugs-atenOLOL, lopresor, OLOL

  1. Calcium channel blockers

  • Inhibit Ca (muscle contraction) from entering heart and blood vessels

  • gingival hyperplasia

  • drugs: nifediPINE (procardia), diltiazem, amlodiPINE, PINE

  1. Diuretics

  • Drugs: hydrochlorothiazIDE, furosemIDE,

Congestive Heart Failure Drug: Digoxin

  1. Pharmacologic effects

  • increases force and strength of heart contractions

  • reduces edema

  1. Uses

  • treatment of HF

  • treatment of arrhthmias

  1. Tip: Digoxin=Deep Contraction=Decreases HR

Anti-Anginal Drugs: Nitroglycerin

  • management of acute anginal episodes

  • prevent anginal attacks induced by stress or exercise

  • vasodilator

  • SL NTG

  • SL isosorbide dinitrate

  • Emergency drug

Anticoagulants:

  • drugs that interfere with coagulation

  • blood thinner

  • given in an attempt to prevent clotting

  • Warfarin (Coumadin) used after a MI or thrombophlebitis

  • Aspirin-anti platelet

  • Clopidogrel (Plavix)

Pain Drugs: Non-opioids and Opioids

Non Opioids:

  1. NSAIDS

  • Ibuprofen (Advil, Motrin)- antipyretic, analgesic, anti-inflammatory

  • Naproxen (Aleve)-antipyretic, analgesic, anti-inflammatory

  1. Acetaminophen (Tylenol)

  • Antipyretic, analgesic, NOT anti-inflammatory

  1. Aspirin (salicylic acid)

  • anti-platelet

  • antipyretic, analgesic, anti-inflammatory

  • could be used for arthritis and cardiovascular diseases

  • not for peeps with acid stomach issues

Opiods:

  1. Codeine

  • Tylenol #3

  • Most commonly used in dentistry

  1. Morphine

  2. Oxycodone

  3. Bind to to three opioid receptors (Mu, Kappa, Delta)

  4. Depresses the CNS and stops pain

  5. Pharmacologic actions-analgesia, cough suppression, sedation and euphoria

Mechanism of action of nonopioid analgesics (prostaglandins, cox II)

Acetylsalicylic Acid: Mechanism of Action (ASA Aspirin)

  • inhibit prostaglandin synthesis

  • enzyme cyclo-oxygenase (COX I and II)

  • Prostaglandins can

  1. sensitize pain receptors

  2. lower pain threshold to painful stimuli

  3. cause inflammation and fever

  4. affects vascular tone and permeability

The Drug of Choice for Inflammatory Dental Pain is IBUPROFEN

The medication is contraindicated with aspirin is WARFARIN

Adverse effects of Opioids: Respiratory Depression

  • cause of death with overdose

  • elderly-decrease in pulmonary ventilation

  • reduced ventilation produces vasodilation

  • vasodilation results in intracranial pressure

  • mask CNS diagnostic symptoms

  • hyperthyroidism

  • hypothyroidism

Treatment Opioid Addiction

  • substituting oral opioid for injectable form

  • cold turkey

  • methadone maintenance

  • administering Naltroxen (Trexan) ; opioid antagonist

Specific Opioid Analgesics and Antagonists:

  1. Opioid agonists

  • Morphine

  • Oxycodone

  • Oxymorphone

  • Hydrocodone

  • Codeine

  • meperidine

  • Hydromorphone

  • Methadon

  • Fentanyl family

Superinfection: Suprainfection

  • infection occurring after or on top of an earlier infection, especially following treatment with broad spectrum antibiotics (candidiasis after antibiotic use)

  • can be minimized by use of the most specific anti-infective agent, the shortest effective course of therapy, and enough doses

Antibiotic prophylaxis used in dentistry:

  • prosthetic cardiac valve

  • previous infective endocarditis

  • congenital heart disease (CHD)

Preventive antibiotic regimen for adults:

  • 2g amoxicillin 1 hr prior to appointment

  1. If patient is allergic to penicillin use:

  • 600 mg clindamycin 1 hr prior to appointment

  • 500 mg azithromycin 1 hr prior to appointment

  • 500 mg clarithromycin 1hr prior to appointment

Anti-viral agents: Infections lesions: Herpes

  • self limiting to the patient with normal immunity

  • HSV 1= oral

  • HSV 2=genital

  • Treatment

  1. antiviral agents: acyclovir, valacyclovir, penciclovir (topical only, reduces lesion duration and viral shedding by ½ day), docosanol (no prescription, reduces lesion duration and viral shedding by ½ day)

  2. topical diphenhydramine (Benadryl) or viscous lidocaine

  3. Kaopectate, Maalox Quick Dissolve, Mylanta Gas, Orabase plain or with benzocaine

  • according to the CDC, pts with active herpetic lesions can be treated provided that they are either emergency dental care or the treatment of the lesions only. All other care should be delayed

Antifungal agents: Nystatin for thrush

  • used for both treatment and prevention of thrush

  • cariogenic

  • sucrose content

  • lozenges

  • dentures

  • mechanism of action-binding to sterols in the fungal cell membrane

  • not absorbed from mucous membranes or intact skin

  • poorly absorbed from GI tract

  • excreted unchanged in the feces

  • fungicidal and fungistatic

Antifungal agents for thrush: Imidazoles

  • useful in dentistry (Clotrimazole/Mycelex and ketoconazole/nizoral)

  • Other-fluconazole (diflucan)

GI Diseases:

  1. Ulcers

  • Causes- Helicobacter pylori and use of NSAIDs

  • Treatment-combo of one or more antibiotics and an H2 blocker or a PPI to reduce stomach acid

  • Histamine2 Blocking agents-block and inhibit gastric acid secretion by competitive inhibition of histamine at the H2 receptors of parietal cells: Cimetidine (Tagamet) is the prototype, Famotidine, Ranitidine, Nizatidine

  • Proton Pump Inhibitors PPIS Side Effects-headache, diarrhea (C. difficile), nausea, dizziness, mucosal atrophy of tongue, dry mouth, osteoportic fractures, gastroduodenal tumors

  1. GERD

Antiemetics: drugs used to induce vomiting and to prevent vomiting

  • Phenothiazines (prochlorperazine)

  • Promethazine

Laxative: constipation

  1. Bulk laxatives-pros (safest, act the most like normal physiology)

  2. Lubricants-cons (interfere with absorption of fat soluble vitamins)

  3. Stimulants-cons (intestinal cramping)

  4. Stool softeners-Pros ( nontoxic)

  5. Osmotic (saline) laxative-caution in peeps with renal implants

Antipsychotic Agents:

  1. Mechanism of Action

  • 1st gen-dopamine antagonists

  • 2nd gen-action at more than one receptor

  • Slowing of psychomotor activity

  • calming of emotion

  • suppression of hallucinations and delusions

  • antiemetic

Best non-narcotic analgesic for the management of a dental pt with peptic ulcer disease or GERD is ACETAMINOPHEN

Antidepressant Agents:

  • Electroconvulsive therapy (ECT)

  1. Fastest results seen with depression

  2. Reserved for pts who are refractive to antidepressants

  • Selective serotonin reuptake inhibitors (SSRIs)

  1. Fluoxetine (Prozac), citalopram (Celexa)

  • Serotonin norepinephrine reuptale inhibitors (SNRIs)

  • Tricyclic antidepressants (TCAs)

  1. Amitriptyline (Elavile)

  • Other agents

Anti-anxiety Agents:

  • reduce anxiety, treat seizures, induce sleep

  • side effect-xerostomia

  • drugs used:

  1. Benzodiazepines-reduced anxiety, anticonvulsants, muscle relaxants

  2. Diazepam (Valium), lorazepam (Ativan), alprazolam (Xanax)

  3. End in ZEPAM, ZOLAM

Anti-convulsants: Phenytoin

  • gingival enlargement symptoms

  1. often painless enlargement of the gingival margin

  2. interproximal papillae involvement

  3. coalesce to cover occlusal surfaces of the teeth

  • prevention-oral hygiene, home care

Asthma:

  • reversible airway obstruction

  • linked with reductio in expiratory airflow

  • allergens

  • exercise

  • stress

  • URT infection

  • environmental pollution

  • signs-wheezing

COPD:

  • irreversible airway obstruction

  • chronic bronchitis is a result of chronic inflammation of the airways and excessive sputum production

  • emphysema is characterized by alveolar destruction with airspace enlargement and airway collapse

Metered-dose inhalers (MDIS)

  • Pros

  1. med delivered directly into bronchioles

  2. bronchodilator effect is greater than oral dose

  3. inhaled dose can be accurately measured

  4. rapid and predictable onset of action

  5. compact, portable, and sterile

Sympathomimetic or adrenergic agents for asthma and copd

  • Inhaled short acting B2 agonists (asthma and copd_

  1. Albuterol (Ventolin, ProAir HFA, Proventil)

  2. Metaproterenol

  3. Levelbuterol

  • Inhaled short acting B2 agonists/short acting anticholinergic combos (COPD)= Albuterol/Ipratropium

Sympathomimetic or Adrenergic agents for persistent asthma

  • Inhaled acting B2 agonists

  1. Salmeterol

  2. Budesonide/formoterol

  3. Mometason/formoterol

  • Used with low does corticosteroids to treat not well controlled (low dose)

Corticosteroids for asthma

  • hasten recovery and decrease morbidity (reduce hyperreactive airway) despite no immediate benefits in acute asthma attack

  • Inhaled-most effective long term treatment for persistent asthma

  1. Beclomothasone and Fluticasone

  • Oral corticosteroids

  1. Prednisone

  • Adverse effects with chronic use of inhalation

  1. Candidiasis

Local Anesthesia:

  • Ester

  1. metabolized in plasma

  2. allergic

  • Amide

  1. metabolized in liver

  2. no allergic reactions

  3. I before caine

  • Don’t give too much epinephrine to cardiac patients (0.04 mg max dose)

  • healthy patients (.20 mg)

  • not for uncontrolled diabetes

  • carefully if someone is on tricyclic antidepressants

LA Agents:

  • Lidocaine

  1. safe in pregnancy

  2. can have epinephrine or be plain

  • Mepivacaine

  1. can have levonordefrin or plain

  2. used in short in dental procedures if epinephrine is contraindicated

  • Bupivacaine

  1. teratogenic in rats (category C)

  2. slow onset (takes long to kick in)

  3. used for long dental procedure (7 hours!)

Vasoconstrictor:

  • vasodilation when LA

  • epinephrine and levonordefrin (more toxic)

  • constrcition=longer duration

Nitrous Oxide:

  • oxygen for 5 min to prevent diffuse hypoxia

  • relieve anxiety

  • conscious, can follow instructions

  • weak anesthetic agent, pain free, can cause memory loss

  • average peeps needs 35% nitrous oxide in oxygen with a range of 10 to 50%

  • adverse effects: nausea, vomiting

  • NO respiratory depression, bronchodilation or low P

  • Contraindications

  1. COPD

  2. Respiratory obstructions

  3. 1st trimester

  4. bowel obstructions

Immunosuppressant drug:

  • used in organ transplant pts to prevent rejection of organ

  • azathioprine, cyclosporine (gingival enlargement), tacrolimus

Bisphosphonate drugs

  • prevent loss of bone density for osteoporosis, slow tumor development

  • Many cancer pts with pain may take this=can develop osteonecrosis of the jaw

Diabetes:

  • Type I=can’t make insulin (need injections)

  • Type II=can’t make enough or use insulin; metformin, fortamet

  • side effects=hypoglycemia (most common), poor wound healing, weight gain, infections