Antilipemic Drugs

● When dietary fats is taken into the body it is absorbed into our intestine to form
triglycerides and cholesterol
● Triglycerides and cholesterol: two main components of lipid
Cholesterol Homeostasis
● Triglycerides
○ Energy source stored in adipose tissue
● Cholesterol
○ Incorporated into circulating proteins called lipoproteins and is transported from
the intestines to the liver
○ The transportation of cholesterol bound to the protein in the liver will be used for
synthesizing steroids used for endocrine system such as:
■ Bile- for food absorption
■ Cell wall synthesis
○ There are two major mechanism in participation of apolipoprotein receptor and
enzymes:
■ Transport of cholesterol
■ Transport of triglycerides
○ Endogenous substance or "Naturally occuring"
○ Can also be taken from dietary sources such as:
■ Food rich in cholesterol
■ Precursors of cholesterol
○ Condition associated with the increase in Cholesterol:
■ Excess dietary carbohydrates are converted into triglycerides which is a
precursor of cholesterol
■ Hyperlipidemia
● Hyperlipidemia
○ Abnormal elevation of cholesterol and triglyceride level in the body
1. Can be due to genetic disorder
2. Can also be caused by secondary causes:
○ Lifestyle
○ Drugs intake
○ Underlying conditions
● Great contributor of hyperlipidemia: a highly saturated fats, cholesterols,
carbohydrates, as well as alcohol coupled with sedentary lifestyle
● Treatments:
a. Dietary component treatment: includes reduction of weight, exercise
and diet in cholesterol
● According to American heart Association and National Cholesterol
Education Program the recommended fat intake should be <30% of the
calories
b. Drug component treatment
● Niacin- effective in lowering total cholesterol and lowering cholesterol levels particularly
the triglycerides
○ Increases good cholesterol
○ Also known as nicotinic acid, a water soluble vit D that inhibits the VLDL
synthesis using Liver cells causing the decrease of LDL and triglycerides
○ Cheap drug
○ Not recommended to diabetic patient because of the possibility of acquiring
glucose intolerance
● Statin- effective in lowering LDL
● Fibrate-
 ● Bile acid binding resins- drugs that binds the bile in the intestine
○ Used in dietary therapy to reduce cholesterol particularly in type 2
hyperlipidemia
○ Also useful to secondary to partial biliary stasis
Antihypertensive drugs
● Heart facilitates the circulation of the blood to tissues and organs
● Blood Pressure
○ Systolic blood pressure/Arterial blood pressure- heart contraction that
generates pressure when blood is pushed out of the heart
○ Diastolic blood pressure:
○ Pulse pressure: Difference between the diastolic and systolic
● Mean arterial pressure (MAP)
○ The average pressure throughout the heartbeat cycle
○ Preffuses tissue
● Arterial blood pressure
○ Almost synonymous to systolic pressure
○ Product of cardiac output and Peripheral Vascular Resistance
○ Cardiac output (CO)
■ The main systolic blood pressure
● Stroke volume
○ Volume of the blood ejected by tye single contraction of the
left ventricle
○ Indicated as ml/min
■ Average of 4-8 L/m
● Heart Rate
○ Controlled by autonomic nervous system
 ● Venous capacitance
○ Capacity of the veins to return blood to the heart
○ Peripheral vascular resistance (PVR)
Hypertension
● Condition characterized by an elevation of systolic pressure, of diastolic pressure or
both
● Primary hypertension
○ Idiopathic, unknown case
○ Incurable
● Secondary hypertension
○ Occurs with another disorder such as: Diabetic, cushing's syndrome, renal
diseases, trauma

Blood pressure Categories

Hypertension drugs
Preferred Agents
● Diuretics
○ Act by causing volume reduction, sodium excretion, and vasodilation of
peripheral arterioles
○ Most commonly prescribed antihypertensive drugs
○ Classes of Diuretics
■ Carbonic anhydrase inhibitors- has a weak effect
■ Thiazide
■ Loop diuretics

■ Potassium-sparing diuretics: CAn be used alone, usually combined

with Thiazide and Loop diuretics
Blocking Agents
● Inhibit cardiac response to sympathetic nerve stimulation by blocking the beta-receptors
● Produces reduction in heart rate, cardiac output and blood pressure
● Side effects
○ Bradycardia, peripheral vasoconstriction, purpling and mottling of the skin.
○ Bronchospasms, wheezing
○ Diabetic patients: monitored for hypoglycemia
○ Heart failure manifested in edema, dyspnea, bradycardia and orthopnea
ACe Inhibitors
 ● Blocks the conversion of Angiotensin 1 to angiotensin 2

Calcium lon Antagonists

● Inhibit the movement of calcium ions across a cell membrane
○ Major antagonist of calcium ion is: Hypertension and sinup
● Fewer arrhythmias, slower rate of contraction of the heart, relaxation of the smooth
muscle of the blood vessels.
● Classification
○ Benzothiazepines
■ Diltiazem
○ Diaminopropanol ether
■ Bepridil
○ Phenylalkylamines
■ Verapamil
○ Dihydropyridines (pine)
■ Amlodipine
■ Felodipine
■ Isradipine
■ Nifedipine
■ Nimodipine
■ Nisoldipine
Drug for heart Failure
● Systolic Dysfunction
○ Most common cause of heart failure
○ Heart is unable to contract enough force to pump all the blood
○ Decreased cardiac output
○ Enlargement of the left ventricle
● Diastolic Dysfunction
 ○ Left ventricle develops stiffness
■ It fails to relax between contraction
○ Pulmonary congestion
○ Peripheral edema
○ Constrictive pericarditis, ventricular muscle hypertrophy, and valvular heart
disease
● Digoxin
○ Commonly used drug
○ Actions:
■ Positive inotropic response increases the force of contraction
■ Negative chronotropy decreases heart rate
○ Digitalis glycosides
■ Used for treating moderate to severe systolic heart failure that is not
responsive to diuretics and ACE inhibitor
○ Usually used for systolic heart failure, NOT commonly used to diastolic heart
dysfunction

Dosage of Digoxin

Treatment for Digitalis Toxicity

● Occurs in the elderly
● Early symptoms: anorexia and mild nausea
● Changes in Pulse rhythm and rate CNS signs such as mental status, orientation,
changes in color vision, hallucinations, or behavior.
● Children: Atrial Arrhythmias
● Electrolyte imbalance
○ Hypokalemia
■ Corticosteroids
■ Bumetanide
○ Hyperkalemia
 ■ Heparin
■ Beta adrenergic blockers
■ Mannitol infusions
○ Hypomagnesemia
■ Ethanol
■ Furosemide
Antimicrobial Agents
● Microorganism can be found in both internal and external environments
● Normal flora
○ Escherichia coli - intestine
○ Streptococcus - skin
● Chemotherapy
○ Use to kill cancer cells
○ Use of chemicals to treat both cancer and infection
○ Cancer Chemotherapy and Chemotherapy of infectious disease
Antibiotics
● Produced by microorganism
Antimicrobial
● Any agent, synthetic, or natural that can kill or inhibit the growth of microorganisms
● Bacteriostatic
○ Capable of inhibition of the growth of microorganism
● Bactericidal
○ This agent can kill microorganisms
Selective Toxicity
● Ability of the drug to kill or injure a target organism which is disease-inducing
● without injuring other cells within the immediate vicinity.
● Actions:
1. Disruption of the bacterial cell wall
2. Inhibition of enzyme unique to the bacteria
3. Disruption of bacterial protein synthesis
4. Antimetabolite action

Susceptible Microorganism
● Antibacterial
● Antifungal
● Antiviral
● Antiprotozoan
● Antihelminthic

Scope of drug Action

● Narrow spectrum antibiotics
○ Agents that can act against few microorganism
○ Most preferred antibiotics
● Broad spectrum antibiotics
 ○ Wide variety of actions in microorganism

Based of mechanism
● Cell wall inhibitors
○ Promotes kysis of the cell wall
○ Eg. Penicillin
● Increase cell membrane permeability
● Bacterial protein synthesis inhibitor
● DNA and RNA inhibitors
○ Eg Rifampin, Metronidazole, Florotenums
● Antimetabolites
○ Sulfonamides, trimetraphine
● Suppressed viral replication
■ Capable of DNA polymerase, reverse transcriptase, protease,
muramidase
■ Needed for replication infectivity of the virus
Aminoglycoside
● Kills bacteria by inhibiting protein synthesis
● Use against gram-negative bacteria
○ UTI
○ Meningitis
○ Wound infections
○ Septicemias
● Treatment of nosocomial infections
○ Acinetobacter, Citrobacter, Enterobacter, Escherichia coli,
Klebsiella,Providencia, Pseudomonas, Salmonella, and Shigella
● Kanamycin and Neomycin
○ Preoperative reduction of normal flora in the intestine
● Side effects
○ Ototoxicity
■ Damage in the 8th cranial nerve
■ Dizziness, progressive loss of healing
○ Nephrotoxicity
■ Kidney function tests
■ Increase of BUN and Creatinine with a presence of CASTS
● Drug interactions
○ Increase nephrotic potential
○ Increase ototoxic potential
○ Neuromuscular blockade

Dosage of Aminoglycosides
Cephalosporins
● Chemically related to penicillins
● Acts by inhibiting cell wall synthesis
● Generations

● 3rd generation can be used for Pseudomonas aeruginosa

● Side effects
○ Diarrhea
 ○ Secondary Infections
■ Thrush, genital and oral pruritus, and vaginitis
○ Abnormal liver and renal functions
○ Increase AST, ALT and ALP
○ Hypothrombinemia
○ Thrombophlebitis and phlebitis
○ Electrolyte imbalance
Vancomycin
● Prevents the synthesis of bacterial cell wall
● Effective against gram positive bacteria that may cause endocarditis, meningitis,
pneumonia and septicemia
○ Streptococcus
○ Staphylococcus
○ Clostridium
○ Clostridium difficile
○ Listeria monocytogenes
○ Corynebacterium
● PO: 500 mg q 6H or 1g q 12H
● Nephrotoxic
○ Decrease in urine output and production of casts
○ Excessive RBC in the urine
● Ototoxic
○ Urine loss

Antiepileptic drugs
● Epilepsy
○ Generic name that refers to a group of neurologic disorders
○ Characterized by repetitive convulsive seizures, sensory disturbances, abnormal
behavior, loss of consciousness.
● Seizures
○ Indicate abnormalities in the nerve centers of the brain
○ Brief episode of abnormal electrical activity in the brain
○ Can be classified into:
■ Convulsive
● Violent
● Involuntary convulsive contraction
■ Non-convulsive
● Not violent
● Convulsion
○ Involuntary spasmodic contraction of voluntary muscles in the body
○ Facial, skeletal Muscles

EEG- Electroencephalography
● Video monitoring of impulses in the body
Classification of Epilepsy

Antiepileptic Drug
● Control or prevent seizures while maintaining a reasonable comfortable quality of life
● Have many adverse side effects
Barbituates
Drugs for Mood Disorders
● Mood
○ Sustained emotional feeling perceived along continuum of sad
● Mood disorder
○ Affective disorder characterized by abnormal feelings of depression or euphoria
○ Depressive
○ Bipolar Disorder (Manic Depression)
● Types of Depression
○ Mild Depression
○ Severe Depression
○ Moderate Depression

Drug therapy for Mood disorders

● Monoamine Oxidase Inhibitors (MAOIs)
○ Block the metabolic destruction of norepinephrine, dopamine, and serotonin by
monoamine oxidase
○ phenelzine
○ tranylcypromine
○ Isocarboxazid
● Selective Serotonin Reuptake inhibitors (SSRIs)
○ Most widely used because they don't have anticholinergic and cardiovascular
side effects
○ citalopram
○ fluoxetine
○ fluvoxamine
 ○ Paroxetine
● Tricyclic Depressants
○ Prolong the action of norepinephrine, dopamine and serotonin by blocking
reuptake of these neurotransmitters in the synaptic cleft between neurons.
○ amitriptyline
○ amoxapine
○ clomipramine
○ desipramine
○ doxepin
○ imipramine
● Lithium
○ Monovalent cation that competes with potassium, calcium, sodium and
magnesium ions at cellular binding sites sensitive to changes in cation
concentrations.
○ Antimanic agent for adults
○ Drug for Bipolar disorder
○ Used to stabilize neural membrane
○ Releases norepinephrine and increase tryptophan
○ Nausea, vomiting, tremors, anorexia, diarrhea, liturgy
○ Adverse effects: progessive fatigue, weight gain, ankle edema, hyperglycemia
and nephrotoxicity