International Journal of Endocrinology / 2018 / Article / Tab 2

Review Article

Drugs Involved in Dyslipidemia and Obesity Treatment: Focus on Adipose Tissue

Table 2

Drugs used in obesity: classical effects, effects on adipose tissue, and weight.

Drugs used in obesityClassical mechanism of actionAdipose tissue effectsAppetite regulation
AT mass/AT depotsGlucose metabolism/insulin sensitivityLipid metabolismAdipocytokine expressionAntiatherogenicAdipogenesisBrowning effectAnti-inflammatory

OrlistatReversible inhibitor of gastric and pancreatic lipase⊕ [159, 160]⊕ lipolysis [160]Leptin [160]
SibutramineSympathomimetic amine; inhibition of NA and 5-HT reuptake↓ TG [164]
↑ HDL [164]
Adiponectin [164]Leptin and resistin [164]↓ CRP [164]
DiethylpropionSympathomimetic amine; inhibition of NA, 5-HT; DA reuptake⊝ [165]
PhentermineSympathomimetic amine; noradrenergic modulation; DA receptor agonist⊝ and promotes saciety [166]
Lorcaserin5-HT2c receptor agonist⊝ and promotes saciety [167, 168]
Naltrexone and bupropionAntagonist of opioid receptors in POMC neurons and inhibitor of reuptake of NA and DA↓, mainly VAT [170]
TopiramateAntagonist of AMPA receptors and stimulation of GABA receptors⊕ [171]Adiponectin [171]Leptin [172]⊕ UCP 2/3 expression [172]⊝ [172]
LiraglutideGLP-1R agonist↓ [175, 182188]; mainly VAT [175178, 182187]⊕ [178, 182, 185, 192]⊕ FA oxidation [182, 188]; ⊝ lipogenesis [176]Adiponectin (in dysfunctional adipocyte) [189, 197];
omentin [192]
TNFα [181]↓ CRP and sICAM-1 levels [175]⊕ [194]⊕ [180, 182, 188]Vide adipokine regulation⊝ and promotes saciety and improves eating behaviour [175180]

⊕: stimulates; ⊝: inhibits; AT: adipose tissue; TG: triglycerides; HDLs: high-density lipoproteins; CRP: C-reactive protein; NA: noradrenaline; 5-HT: 5-hydroxytryptamine; DA: dopamine; POMC neurons: pro-opiomelanocortin neurons; VAT: visceral AT; AMPA receptors: a-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptors; GABA receptors: γ-aminobutyric acid receptors; FA: fatty acid; TNFα: tumour necrosis factor α; GLP-1R: glucagon-like peptide 1 receptor; sICAM-1: soluble intracellular adhesion molecule-1.